Thiazole derivatives in medicinal chemistry: Recent advancements in synthetic strategies, structure activity relationship and pharmacological outcomes

Cancer statistics, 2022

(2022) Rebecca L. Siegel et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Design, synthesis, and biological evaluation of isatin‐indole‐3‐carboxaldehyde hybrids as a new class of xanthine oxidase inhibitors

(2022) Atamjit Singh et al.   ARCHIV DER PHARMAZIE

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

(2021) Anca-Maria Borcea et al.   MOLECULES

Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents

(2021) Rizk E. Khidre et al.   Scientific Reports

Antiproliferative activity of thiazole and oxazole derivatives: A systematic review of in vitro and in vivo studies

(2021) Nancy Y. Guerrero-Pepinosa et al.   BIOMEDICINE & PHARMACOTHERAPY

Design, synthesis and anti-influenza virus activity of furan-substituted spirothiazolidinones

(2021) Çağla Begüm Apaydın et al.   BIOORGANIC CHEMISTRY

Insights into the structure activity relationship of nitrogen-containing heterocyclics for the development of antidepressant compounds: An updated review

(2021) Karanvir Singh et al.   JOURNAL OF MOLECULAR STRUCTURE

Recent advances on drug development and emerging therapeutic agents for Alzheimer’s disease

(2021) Teeba Athar et al.   MOLECULAR BIOLOGY REPORTS

Comparative study of cefixime and tetracycline as an evaluation policy driven by the antibiotic resistance crisis in Indonesia

(2021) Danni Ramdhani et al.   Scientific Reports

Cefdinir and β-Lactamase Inhibitor Independent Efficacy Against Mycobacterium tuberculosis

(2021) Shashikant Srivastava et al.   Frontiers in Pharmacology

Ixabepilone: Overview of Effectiveness, Safety, and Tolerability in Metastatic Breast Cancer

(2021) Nuhad K. Ibrahim   Frontiers in Oncology

Cefiderocol-Based Combination Therapy for “Difficult-to-Treat” Gram-Negative Severe Infections: Real-Life Case Series and Future Perspectives

(2021) Davide Fiore Bavaro et al.   Antibiotics-Basel

Design, synthesis, and biological evaluation of novel morpholinated isatin–quinoline hybrids as potent anti‐breast cancer agents

(2021) Atamjit Singh et al.   ARCHIV DER PHARMAZIE

The clinical and microbiological efficacy of temocillin versus cefotaxime in adults with febrile urinary tract infection, and its effects on the intestinal microbiota: a randomised multicentre clinical trial in Sweden

(2021) Charlotta Edlund et al.   LANCET INFECTIOUS DISEASES

Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes

(2020) Mohammed T.-E. Maghraby et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of 4-hydroxy-2-oxo-1,2-dihydroquinolines as potential inhibitors of Streptococcus pneumoniae, including drug-resistant strains

(2020) Srigouri Huddar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drug-Like Property Optimization: Discovery of Orally Bioavailable Quinazoline-Based Multi-Targeted Kinase Inhibitors

(2020) Shu-Yu Lin et al.   BIOORGANIC CHEMISTRY

Synthesis, Anti-convulsant activity and Molecular Docking Study of novel Thiazole Pyridazinone Hybrid Analogues

(2020) Aness Ahmad Siddiqui et al.   BIOORGANIC CHEMISTRY

Novel pyrazine based anti-tubercular agents: Design, synthesis, biological evaluation and in silico studies

(2020) Nayera W. Hassan et al.   BIOORGANIC CHEMISTRY

Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency

(2020) Jaime Franco et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Oxadiazolylthiazoles as novel and selective antifungal agents

(2020) Mohamed Hagras et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluation of phenylthiazole and phenylthiophene pyrimidindiamine derivatives targeting the bacterial membrane

(2020) Tingting Fan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, antitumor activity and theoretical calculation of novel PI3Ka inhibitors

(2020) Ru-Yi Jin et al.   BIOORGANIC CHEMISTRY

Discovery of thiazole-based-chalcones and 4-hetarylthiazoles as potent anticancer agents: Synthesis, docking study and anticancer activity

(2020) Thoraya A. Farghaly et al.   BIOORGANIC CHEMISTRY

Key Takeaways From the U.S. CDC’s 2019 Antibiotic Resistance Threats Report for Frontline Providers

(2020) Sameer S. Kadri   CRITICAL CARE MEDICINE

Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy

(2020) Shih-Hsien Chuang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, modelling and molecular docking of new 5-arylazo-2-chloroacetamido thiazole derivatives as antioxidant agent

(2020) Aisha SM. Hossan   JOURNAL OF MOLECULAR STRUCTURE

Synthesis and antimicrobial evaluation of new thiazolyl-1,2,3-triazolyl-alcohol derivatives

(2020) Shivaji Jagadale et al.   MEDICINAL CHEMISTRY RESEARCH

Assessment of Deaths From COVID-19 and From Seasonal Influenza

(2020) Jeremy Samuel Faust et al.   JAMA Internal Medicine

Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt

(2020) Christian Gege et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach

(2020) Christoph Steeneck et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The rational design, synthesis, and antimicrobial investigation of 2-Amino-4-Methylthiazole analogues inhibitors of GlcN-6-P synthase

(2020) Abdelsattar M. Omar et al.   BIOORGANIC CHEMISTRY

Dual mechanisms suppress meloxicam bioactivation relative to sudoxicam

(2020) Dustyn A. Barnette et al.   TOXICOLOGY

Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects

(2020) Ning Chen et al.   Frontiers in Pharmacology

New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation

(2020) Atamjit Singh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and molecular modeling of novel bio-functional moieties derived from 2-cyanoacetamide-3,4,5-substituted thiophene as human carcinoma growth inhibitors

(2020) Mohamed E. Khalifa   JOURNAL OF MOLECULAR STRUCTURE

Lopinavir–ritonavir in patients admitted to hospital with COVID-19 (RECOVERY): a randomised, controlled, open-label, platform trial

(2020) Peter W Horby et al.   LANCET

Discovery of 2-phenylthiazole-4-carboxylic acid, a novel and potent scaffold as xanthine oxidase inhibitors

(2019) Xue Xu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

New thiazol-hydrazono-coumarin hybrids targeting human cervical cancer cells: Synthesis, CDK2 inhibition, QSAR and molecular docking studies

(2019) Somaia S. Abd El-Karim et al.   BIOORGANIC CHEMISTRY

Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors

(2019) Weiyang Dai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma

(2019) Xiaojing Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors

(2019) Xiaofeng Guo et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Design and synthesis of aminothiazole based Hepatitis B Virus (HBV) capsid inhibitors

(2019) Ting Pan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thiazolyl-pyrazole derivatives as potential antimycobacterial agents

(2019) Sushma J. Takate et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The impact of binding site waters on the activity/selectivity trade-off of Janus kinase 2 (JAK2) inhibitors

(2019) Attila Egyed et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

(2019) Krisztián Tóth et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and fungicidal activity evaluation of novel pyrimidinamine derivatives containing phenyl-thiazole/oxazole moiety

(2019) Zhongzhong Yan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, anticancer effect and molecular modeling of new thiazolylpyrazolyl coumarin derivatives targeting VEGFR-2 kinase and inducing cell cycle arrest and apoptosis

(2019) Tahia K. Mohamed et al.   BIOORGANIC CHEMISTRY

Synthesis and structure-activity relationship of tyrosinase inhibiting novel bi-heterocyclic acetamides: Mechanistic insights through enzyme inhibition, kinetics and computational studies

(2019) Abdul Rehman Sadiq Butt et al.   BIOORGANIC CHEMISTRY

Synthesis and structure-activity relationship of elastase inhibiting novel ethylated thiazole-triazole acetamide hybrids: Mechanistic insights through kinetics and computational contemplations

(2019) Abdul Rehman Sadiq Butt et al.   BIOORGANIC CHEMISTRY

Design, synthesis and molecular docking of pyrazolo [3,4d] thiazole hybrids as potential anti-HIV-1 NNRT inhibitors

(2019) H.M. Kasralikar et al.   BIOORGANIC CHEMISTRY

Pharmacological investigation of quinoxaline-bisthiazoles as multitarget-directed ligands for the treatment of Alzheimer’s disease

(2019) Sneha R. Sagar et al.   BIOORGANIC CHEMISTRY

The in vivo antinociceptive and μ-opioid receptor activating effects of the combination of N-phenyl-2′,4′-dimethyl-4,5′-bi-1,3-thiazol-2-amines and naloxone

(2019) Shu-Yu Lin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of aminothiazolyl norfloxacin analogues as potential antimicrobial agents and their biological evaluation

(2019) Liang-Liang Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A novel, potent, and orally bioavailable thiazole HCV NS5A inhibitor for the treatment of hepatitis C virus

(2019) Teng-Kuang Yeh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching

(2019) Alberto Leoni et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models

(2019) William Nguyen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identifying novel anti-osteoporosis leads with a chemotype-assembly approach

(2019) Chao Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, molecular docking and biological screening of N-ethyl-N-methylbenzenesulfonamide derivatives as effective antimicrobial and antiproliferative agents

(2019) Shimaa M. Abd El-Gilil   JOURNAL OF MOLECULAR STRUCTURE

Gentamicin compared with ceftriaxone for the treatment of gonorrhoea (G-ToG): a randomised non-inferiority trial

(2019) Jonathan D C Ross et al.   LANCET

Synthesis and antimycobacterial evaluation of new 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-4-methyl-2-arylthiazole derivatives

(2019) Vikas Shinde et al.   MEDICINAL CHEMISTRY RESEARCH

Design, synthesis, bioactivity, and DFT calculation of 2-thiazolyl-hydrazone derivatives as influenza neuraminidase inhibitors

(2019) Man-Ying Cui et al.   MEDICINAL CHEMISTRY RESEARCH

Neurological, Psychiatric, and Biochemical Aspects of Thiamine Deficiency in Children and Adults

(2019) Shibani Dhir et al.   Frontiers in Psychiatry

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2)

(2019) Erik de Heuvel et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors

(2019) Meng Lei et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones

(2019) Emmanuel O. Olawode et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, fungicidal activity and SAR of 3,4-dichloroisothiazole-based cycloalkylsulfonamides

(2019) Yumeng Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and carbonic anhydrase inhibition activity of benzenesulfonamide-linked novel pyrazoline derivatives

(2019) Alaa A.-M. Abdel-Aziz et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of Trinary Benzocoumarin-Thiazoles-Azomethines derivatives as Effective and Selective Inhibitors of Alkaline Phosphatase

(2019) Pervaiz Ali Channar et al.   BIOORGANIC CHEMISTRY

Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies

(2019) Mahmoud F. Abo-Ashour et al.   BIOORGANIC CHEMISTRY

Thiazolidinone/thiazole based hybrids – New class of antitrypanosomal agents

(2019) Anna Kryshchyshyn et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, in vitro assays, molecular docking, theoretical ADMET prediction, and evaluation of 4-methoxy-phenylthiazole-2-amine derivatives as acetylcholinesterase inhibitors

(2019) Xiao-Zhong Zhang et al.   MEDICINAL CHEMISTRY RESEARCH

Discovery of 3-(thiophen/thiazole-2-ylthio)pyridine derivatives as multitarget anticancer agents

(2019) Jiankang Zhang et al.   MEDICINAL CHEMISTRY RESEARCH

Low-dose ritonavir-boosted darunavir once daily versus ritonavir-boosted lopinavir for participants with less than 50 HIV RNA copies per mL (WRHI 052): a randomised, open-label, phase 3, non-inferiority trial

(2019) Willem D F Venter et al.   Lancet HIV

Design, Synthesis, Antimicrobial Evaluation, and Molecular Modeling Studies of Novel Indolinedione–Coumarin Molecular Hybrids

(2019) Kavita Bhagat et al.   ACS Omega

Monocarbonyl Curcumin-Based Molecular Hybrids as Potent Antibacterial Agents

(2019) Atamjit Singh et al.   ACS Omega

Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors

(2019) Gibeom Nam et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit

(2019) Yuichi Sami et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Thiazolidinedione and thiazole derivatives potentiate norfloxacin activity against NorA efflux pump over expression in Staphylococcus aureus 1199B strains

(2019) Pedro Silvino Pereira et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Thiazole orange – Spermine conjugate: A potent human telomerase inhibitor comparable to BRACO-19

(2019) Siwen Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of bromophenol-thiazolylhydrazone hybrids inhibiting the interaction of translation initiation factors eIF4E/eIF4G as multifunctional agents for cancer treatment

(2019) Lijun Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel 99mTc-2-arylimidazo[2,1-b]benzothiazole derivatives as SPECT imaging agents for amyloid-β plaques

(2019) Sajjad Molavipordanjani et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines

(2019) Xiaofeng Guo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity

(2019) Mohamed M. Elsebaei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of tropinone-thiazole derivatives as potent caspase 3/7 activators, and noncompetitive tyrosinase inhibitors with high antiproliferative activity: Rational design, one-pot tricomponent synthesis, and lipophilicity determination

(2019) Katarzyna Piechowska et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis

(2019) Uttam B. Karale et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and evaluation of new pyrazoline‐thiazole derivatives as monoamine oxidase inhibitors

(2019) Ulviye Acar Çevik et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Bleomycin use in the treatment of Hodgkin lymphoma (HL): toxicity and outcomes in the modern era

(2019) Kekoa Taparra et al.   LEUKEMIA & LYMPHOMA

Chemical synthesis, molecular modeling and pharmacophore mapping of new pyrrole derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth

(2019) Shrinivas D. Joshi et al.   MEDICINAL CHEMISTRY RESEARCH

Synthesis, antimicrobial activity, and determination of the lipophilicity of ((cyclohex-3-enylmethylene)hydrazinyl)thiazole derivatives

(2019) Anna Biernasiuk et al.   MEDICINAL CHEMISTRY RESEARCH

Recent Advances in Exploration and Biotechnological Production of Bioactive Compounds in Three Cyanobacterial Genera: Nostoc, Lyngbya, and Microcystis

(2019) Nguyen Huy Thuan et al.   Frontiers in Chemistry

Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors

(2019) Baijayantimala Swain et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of new triazole fused imidazo[2,1-b]thiazole hybrids with emphasis on Staphylococcus aureus virulence factors

(2019) Mohd Adil Shareef et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

ω-Quinazolinonylalkyl aryl ureas as reversible inhibitors of monoacylglycerol lipase

(2019) Florian M. Dato et al.   BIOORGANIC CHEMISTRY

Design, synthesis, and biological evaluation of novel dual FFA1 (GPR40)/PPARδ agonists as potential anti-diabetic agents

(2019) Zheng Li et al.   BIOORGANIC CHEMISTRY

Synthesis and antibacterial evaluation of a novel library of 2-(thiazol-5-yl)-1,3,4-oxadiazole derivatives against methicillin-resistant Staphylococcus aureus (MRSA)

(2019) Mohamed H. Hannoun et al.   BIOORGANIC CHEMISTRY

New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study

(2019) Fazal Rahim et al.   BIOORGANIC CHEMISTRY

Synthesis, characterization and molecular docking of some novel hydrazonothiazolines as urease inhibitors

(2019) Muhammad Tariq Shehzad et al.   BIOORGANIC CHEMISTRY

Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies

(2019) Dongdong Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A new exploration towards aminothiazolquinolone oximes as potentially multi-targeting antibacterial agents: Design, synthesis and evaluation acting on microbes, DNA, HSA and topoisomerase IV

(2019) Liang-Liang Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of new thiazolyl-pyrazolyl-1,2,3-triazole derivatives as potential antimicrobial agents

(2019) Jitendra Nalawade et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties

(2019) Aya E. Ghonim et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

2-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity

(2019) Marcos Veríssimo de Oliveira Cardoso et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors

(2019) Belgin Sever et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Substituted 4-phenylthiazoles: Development of potent and selective A1, A3 and dual A1/A3 adenosine receptor antagonists

(2019) Aliaa Abdelrahman et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Exploration and Development of PPAR Modulators in Health and Disease: An Update of Clinical Evidence

(2019) Cheng et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy

(2019) Thilo Focken et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effect of Modifier Structure on the Activation of Leukotriene A4 Hydrolase Aminopeptidase Activity

(2019) Kyung Hyeon Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors

(2019) Sandra Röhm et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and characterization for novel Cu(II)-thiazole complexes-dyes and their usage in dyeing cotton to be special bandage for cancerous wounds

(2019) Nashwa El-Metwaly et al.   JOURNAL OF MOLECULAR STRUCTURE

Novel highly functionalized 1,4-naphthoquinone 2-iminothiazole hybrids: Synthesis, photophysical properties, crystal structure, DFT studies, and anti(myco)bacterial/antifungal activity

(2019) Muge Gemili et al.   JOURNAL OF MOLECULAR STRUCTURE

Synthesis, inhibition studies against AChE and BChE, drug-like profiling, kinetic analysis and molecular docking studies of N-(4-phenyl-3-aroyl-2(3H)-ylidene) substituted acetamides

(2019) Fayaz Ali Larik et al.   JOURNAL OF MOLECULAR STRUCTURE

Synthesis, anticancer, antimicrobial, anti-tuberculosis and molecular docking of heterocyclic N-ethyl-N-methylbenzenesulfonamide derivatives

(2019) Khaled F. Debbabi et al.   JOURNAL OF MOLECULAR STRUCTURE

Thiazole-5-carboxylic acid derivatives as potent xanthine oxidase inhibitors: design, synthesis, in vitro evaluation, and molecular modeling studies

(2019) Gurinder Kaur et al.   MEDICINAL CHEMISTRY RESEARCH

Long-Term, Real-World Safety and Efficacy of Teneligliptin: A Post-Marketing Surveillance of More Than 10,000 Patients with Type 2 Diabetes in Japan

(2019) Takashi Kadowaki et al.   ADVANCES IN THERAPY

Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator

(2019) Ronald J. Hinklin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and antileishmanial evaluation of thiazole orange analogs

(2019) Ahmed Abdelhameed et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Efficient synthesis and cell migration inhibitory effect of substituted benzamidothiazolylpyrazole-capped AWD*I-NH2

(2019) Mian Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists

(2019) Zeping Zuo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Derivatives of pyridine and thiazole hybrid: Synthesis, DFT, biological evaluation via antimicrobial and DNA cleavage activity

(2019) Serpil Eryılmaz et al.   BIOORGANIC CHEMISTRY

4-(4-Chlorophenyl)thiazol-2-amines as pioneers of potential neurodegenerative therapeutics with anti-inflammatory properties based on dual DNase I and 5-LO inhibition

(2019) Andrija Smelcerovic et al.   BIOORGANIC CHEMISTRY

Structure based design, synthesis and in vitro antitumour activity of tiazofurin stereoisomers with nitrogen functions at the C-2′ or C-3′ positions

(2019) Vesna Kojić et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Benzo[b]thiophene-thiazoles as potent anti-Toxoplasma gondii agents: Design, synthesis, tyrosinase/tyrosine hydroxylase inhibitors, molecular docking study, and antioxidant activity

(2019) Beata Rosada et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety as anticancer agents

(2019) Mahsa Ansari et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of triterpenoid thiazoles derived from betulonic acid, dihydrobetulonic acid, and ursonic acid

(2019) Lucie Borková et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness

(2019) Yomna Hosny et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thiazole-containing compounds as therapeutic targets for cancer therapy

(2019) Prabodh Chander Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Disrupting the Conserved Salt Bridge in the Trimerization of Influenza A Nucleoprotein

(2019) Jennifer L. Woodring et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters

(2019) Predrag Kalaba et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, anti-HIV activity, molecular modeling study and QSAR of new designed 2-(2-arylidenehydrazinyl)-4-arylthiazoles

(2019) Amna Rauf et al.   JOURNAL OF MOLECULAR STRUCTURE

Effect of o-difluoro and p-methyl substituents on the structure, optical properties and anti-inflammatory activity of phenoxy thiazole acetamide derivatives: Theoretical and experimental studies

(2019) Hussien Ahmed Khamees et al.   JOURNAL OF MOLECULAR STRUCTURE

Synthesis of Schiff base ligand from N-substituted benzenesulfonamide and its complexes: Spectral, thermal, electrochemical behavior, fluorescence quenching, in vitro-biological and in-vitro cytotoxic studies

(2019) Govindaraj Valarmathy et al.   JOURNAL OF MOLECULAR STRUCTURE

Synthesis, characterization and pharmacological evaluation of 2-aminothiazole incorporated azo dyes

(2019) B.N. Ravi et al.   JOURNAL OF MOLECULAR STRUCTURE

Design, synthesis and biological evaluation of novel N,4-diphenylthiazol-2-amine derivatives

(2019) AfraQuasar A. Nadaf et al.   MEDICINAL CHEMISTRY RESEARCH

Chronic inflammation in the etiology of disease across the life span

(2019) David Furman et al.   NATURE MEDICINE

Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives

(2018) Cleudiomar Inácio Lino et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual or multi-targeting inhibitors: The next generation anticancer agents

(2018) Nulgumnalli Manjunathaiah Raghavendra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, anticancer activity and mechanism of action of new thiazole derivatives

(2018) Temístocles Italo de Santana et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Turning natural products into insecticide candidates: Design and semisynthesis of novel fraxinellone-based N-(1,3-thiazol-2-yl)carboxamides against two crop-threatening insect pests

(2018) Yong Guo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

(2018) Andrew S. Felts et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors

(2018) Hervé Geneste et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of 2-amino-4-phenylthiazole analogues to disrupt myeloid differentiation factor 88 and prevent inflammatory responses in acute lung injury

(2018) Lingfeng Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models

(2018) A.L. Zakharenko et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Effectiveness of empiric aztreonam compared to other beta-lactams for treatment of Pseudomonas aeruginosa infections

(2018) Michael Hogan et al.   Infection and Drug Resistance

Novel stilbene analogues containing thiazole moiety: Synthesis, biological evaluation and docking study

(2018) Qi Lu et al.   JOURNAL OF MOLECULAR STRUCTURE

Synthesis, chemical and biological investigations of new Ru(III) and Se(IV) complexes containing 1,3,5-triazine chelating derivatives

(2018) Fatima A.I. Al-Khodir et al.   JOURNAL OF MOLECULAR STRUCTURE

Thiazole fused thiosemicarbazones: Microwave-assisted synthesis, biological evaluation and molecular docking study

(2018) Neelam P. Prajapati et al.   JOURNAL OF MOLECULAR STRUCTURE

Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents

(2018) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel β-pinene-based thiazole derivatives as potential anticancer agents via mitochondrial-mediated apoptosis pathway

(2018) Yunyun Wang et al.   BIOORGANIC CHEMISTRY

Synthesis of novel N-(1,3-thiazol-2-yl)benzamide clubbed oxadiazole scaffolds: Urease inhibition, Lipinski rule and molecular docking analyses

(2018) Muhammad Athar Abbasi et al.   BIOORGANIC CHEMISTRY

Carbazole and hydrazone derivatives as new competitive inhibitors of tyrosinase: Experimental clues to binuclear copper active site binding

(2018) Usman Ghani   BIOORGANIC CHEMISTRY

Synthesis and anti-proliferative activity of some new quinoline based 4,5-dihydropyrazoles and their thiazole hybrids as EGFR inhibitors

(2018) Riham F. George et al.   BIOORGANIC CHEMISTRY

In vitro and in silico evaluation of new thiazole compounds as monoamine oxidase inhibitors

(2018) Begüm Nurpelin Sağlık et al.   BIOORGANIC CHEMISTRY

Ravuconazole self-emulsifying delivery system: in vitro activity against Trypanosoma cruzi amastigotes and in vivo toxicity

(2017) Pollyanna Álvaro Ferreira Spósito et al.   International Journal of Nanomedicine

Antibacterial and β-Lactamase Inhibitory Activity of Monocyclic β-Lactams

(2017) Lena Decuyper et al.   MEDICINAL RESEARCH REVIEWS

Therapies for acute myeloid leukemia: vosaroxin

(2017) Hamid Sayar et al.   OncoTargets and Therapy

Synthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives

(2016) Umit M. Kocyigit et al.   ARCHIV DER PHARMAZIE

Design, synthesis and antimalarial evaluation of novel thiazole derivatives

(2016) José María Bueno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives

(2016) Subhash Chander et al.   BIOORGANIC CHEMISTRY

Coordination chemistry of thiazoles, isothiazoles and thiadiazoles

(2016) Luís M.T. Frija et al.   COORDINATION CHEMISTRY REVIEWS

Thiazole: A Review on Chemistry, Synthesis and Therapeutic Importance of its Derivatives

(2016) Mahesh T. Chhabria et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Recent applications of 1,3-thiazole core structure in the identification of new lead compounds and drug discovery

(2015) Adile Ayati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Faldaprevir for the Treatment of Hepatitis C

(2015) Tatsuo Kanda et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Simeprevir versus telaprevir with peginterferon and ribavirin in previous null or partial responders with chronic hepatitis C virus genotype 1 infection (ATTAIN): a randomised, double-blind, non-inferiority phase 3 trial

(2015) K Rajender Reddy et al.   LANCET INFECTIOUS DISEASES

Synthesis, biological evaluation and molecular docking studies of thiazole-based pyrrolidinones and isoindolinediones as anticonvulsant agents

(2015) Hazem A. Ghabbour et al.   MEDICINAL CHEMISTRY RESEARCH

Antimicrobial resistance: a global multifaceted phenomenon

(2015) Francesca Prestinaci et al.   Pathogens and Global Health

Ceftaroline in the management of complicated skin and soft tissue infections and community acquired pneumonia

(2015) Mbiye Mpenge et al.   Therapeutics and Clinical Risk Management

Cyclooxygenase-2 selective non-steroidal anti-inflammatory drugs (etodolac, meloxicam, celecoxib, rofecoxib, etoricoxib, valdecoxib and lumiracoxib) for osteoarthritis and rheumatoid arthritis: a systematic review and economic evaluation

(2014) Y Chen et al.   HEALTH TECHNOLOGY ASSESSMENT

Improved Total Synthesis and Biological Evaluation of Potent Apratoxin S4 Based Anticancer Agents with Differential Stability and Further Enhanced Activity

(2014) Qi-Yin Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

A model study on the photochemical isomerization of isothiazoles and thiazoles

(2014) Ming-Der Su   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Nicotinamide mononucleotide adenylyltransferase2 overexpression enhances colorectal cancer cell-kill by Tiazofurin

(2013) P Kusumanchi et al.   CANCER GENE THERAPY

Cobicistat: A Review of Its Use as a Pharmacokinetic Enhancer of Atazanavir and Darunavir in Patients with HIV-1 Infection

(2013) Emma D. Deeks   DRUGS

Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents

(2013) M.H.M. Helal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pramipexole in patients with early Parkinson's disease (PROUD): a randomised delayed-start trial

(2013) Anthony HV Schapira et al.   LANCET NEUROLOGY

Synthesis, anti-inflammatory evaluation, and docking studies of some new thiazole derivatives

(2013) Pran Kishore Deb et al.   MEDICINAL CHEMISTRY RESEARCH

A review on various heterocyclic moieties and their antitubercular activity

(2011) S. Sharma et al.   BIOMEDICINE & PHARMACOTHERAPY

Is cefepime safe for clinical use? A Bayesian viewpoint

(2011) A. C. Kalil   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Terminal Alkene Formation by the Thioesterase of Curacin A Biosynthesis

(2011) Jennifer J. Gehret et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Thiazoles: having diverse biological activities

(2011) Shiv Jee Kashyap et al.   MEDICINAL CHEMISTRY RESEARCH

Larval papulonodular dermatitis treated with topical tiabendazole

(2010) Vincent Lönngren et al.   LANCET INFECTIOUS DISEASES

SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME SUBSTITUTED AMINO THIAZOLE DERIVATIVES

(2010) A. K PRAJAPATI et al.   JOURNAL OF THE CHILEAN CHEMICAL SOCIETY

The H2 Receptor Antagonist Nizatidine is a P-Glycoprotein Substrate: Characterization of its Intestinal Epithelial Cell Efflux Transport

(2009) Arik Dahan et al.   AAPS Journal

Participation of mitochondrial respiratory complex III in neutrophil activation and lung injury

(2009) Jaroslaw W. Zmijewski et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Discovery of 4-Substituted Methoxybenzoyl-aryl-thiazole as Novel Anticancer Agents: Synthesis, Biological Evaluation, and Structure−Activity Relationships

(2009) Yan Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Famotidine for the prevention of peptic ulcers and oesophagitis in patients taking low-dose aspirin (FAMOUS): a phase III, randomised, double-blind, placebo-controlled trial

(2009) Ali S Taha et al.   LANCET

Synthesis, Antibacterial Activity of 2,4-Disubstituted Oxazoles and Thiazoles as Bioisosteres

(2009) Mohamed Kaspady et al.   Letters in Drug Design & Discovery

Modes of Action of the New Arylguanidine Abafungin beyond Interference with Ergosterol Biosynthesis and in vitro Activity against Medically Important Fungi

(2008) C. Borelli et al.   CHEMOTHERAPY

Imidazo[2,1-b]thiazole System: A Scaffold Endowing Dihydropyridines with Selective Cardiodepressant Activity

(2008) Roberta Budriesi et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Neglected Tropical Diseases of Latin America and the Caribbean: A Review of Disease Burden and Distribution and a Roadmap for Control and Elimination

(2008) Peter J. Hotez et al.   PLoS Neglected Tropical Diseases