Pyrimidine derivatives with antitubercular activity

Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies

(2021) Candice Soares de Melo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationships of Pyrazolo[1,5-a]pyrimidin-7(4H)-ones as Antitubercular Agents

(2021) Sangmi Oh et al.   ACS Infectious Diseases

Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 inhibitors TBA-7371, PBTZ169 and OPC-167832

(2021) Gregory T. Robertson et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

First-in-Human Evaluation of the Safety, Tolerability, and Pharmacokinetics of SPR720, a Novel Oral Bacterial DNA Gyrase (GyrB) Inhibitor for Mycobacterial Infections

(2021) Angela K. Talley et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors

(2021) Lijun Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

An Outline of the Latest Crystallographic Studies on Inhibitor-Enzyme Complexes for the Design and Development of New Therapeutics against Tuberculosis

(2021) Matteo Mori et al.   MOLECULES

The quest for the holy grail: new antitubercular chemical entities, targets and strategies

(2020) Stanislav Huszár et al.   DRUG DISCOVERY TODAY

Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity

(2020) Jennifer A. Borthwick et al.   JOURNAL OF MEDICINAL CHEMISTRY

OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor

(2020) Norimitsu Hariguchi et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Tracking total spending on tuberculosis by source and function in 135 low-income and middle-income countries, 2000–17: a financial modelling study

(2020) Yanfang Su et al.   LANCET INFECTIOUS DISEASES

Endeavors towards transformation of M. tuberculosis thymidylate kinase (MtbTMPK) inhibitors into potential antimycobacterial agents

(2020) Yanlin Jian et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo[1,5-a]pyrimidine analogues as potential anti-tubercular agents

(2019) Palmi Modi et al.   BIOORGANIC CHEMISTRY

Synthesis, biological evaluation and computational study of novel isoniazid containing 4H-Pyrimido[2,1-b]benzothiazoles derivatives

(2019) Manoj N. Bhoi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-N1)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism

(2019) Wenhe Zhong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of 4-Amino-Thieno[2,3-d]Pyrimidines as QcrB Inhibitors in Mycobacterium tuberculosis

(2019) Gregory A. Harrison et al.   mSphere

In Vitro Susceptibility of Mycobacterium tuberculosis to Amikacin, Kanamycin, and Capreomycin

(2018) J. A. Dijkstra et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors

(2018) Lijun Song et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis

(2018) Rupesh V. Chikhale et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of N-Benzyl 3,5-Dinitrobenzamides Derived from PBTZ169 as Antitubercular Agents

(2018) Linhu Li et al.   ACS Medicinal Chemistry Letters

Synthesis and biological evaluation of 1H-pyrrolo[2,3-d]pyrimidine-1,2,3-triazole derivatives as novel anti-tubercular agents

(2018) Kasa Shiva Raju et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and Structure–Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2′-Oxidase

(2018) Sangmi Oh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of novel pyrimidine derivatives as potent antitubercular agents

(2018) Pingxian Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and antimycobacterial activity of novel imidazo[1,2- a ]pyridine-3-carboxamide derivatives

(2017) Kai Lv et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent advances of pyrazole-containing derivatives as anti-tubercular agents

(2017) Zhi Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Influence of the charge of the complex unit on the SCO properties in pyrazolyl-pyridinyl-benzimidazole based Fe(II) complexes

(2017) C. Rajnák et al.   POLYHEDRON

Elaboration of a proprietary thymidylate kinase inhibitor motif towards anti-tuberculosis agents

(2016) Lijun Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of N-(2-Phenoxyethyl)imidazo[1,2-a]pyridine-3-carboxamides as New Antituberculosis Agents

(2016) Zhaoyang Wu et al.   ACS Medicinal Chemistry Letters

Novel benzothiazole containing 4H-pyrimido[2,1-b]benzothiazoles derivatives: One pot, solvent-free microwave assisted synthesis and their biological evaluation

(2016) Manoj N. Bhoi et al.   Arabian Journal of Chemistry

A Novel Antimycobacterial Compound Acts as an Intracellular Iron Chelator

(2015) Marte S. Dragset et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis

(2015) Benoit Lechartier et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The Complex Mechanism of Antimycobacterial Action of 5-Fluorouracil

(2015) Vinayak Singh et al.   CHEMISTRY & BIOLOGY

2-Substituted 6-(Het)aryl-7-deazapurine Ribonucleosides: Synthesis, Inhibition of Adenosine Kinases, and Antimycobacterial Activity

(2015) Vincent Malnuit et al.   ChemMedChem

Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides

(2015) Rupesh Chikhale et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Validation of a homology model of Mycobacterium tuberculosis DXS: rationalization of observed activities of thiamine derivatives as potent inhibitors of two orthologues of DXS

(2015) T. Masini et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Whole Cell Target Engagement Identifies Novel Inhibitors of Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase

(2015) Sarah M. Batt et al.   ACS Infectious Diseases

Towards a new combination therapy for tuberculosis with next generation benzothiazinones

(2014) V. Makarov et al.   EMBO Molecular Medicine

Multidrug-Resistant Tuberculosis and Culture Conversion with Bedaquiline

(2014) Andreas H. Diacon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Fueling Open-Source Drug Discovery: 177 Small-Molecule Leads against Tuberculosis

(2013) Lluís Ballell et al.   ChemMedChem

Kinetic mechanism and inhibition ofMycobacterium tuberculosisd-alanine:d-alanine ligase by the antibioticd-cycloserine

(2013) Gareth A. Prosser et al.   FEBS Journal

The Temperature Sensitivity of a Mutation in the Essential tRNA Modification Enzyme tRNA Methyltransferase D (TrmD)

(2013) Isao Masuda et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective Inhibitors of Bacterial t-RNA-(N1G37) Methyltransferase (TrmD) That Demonstrate Novel Ordering of the Lid Domain

(2013) Pamela J. Hill et al.   JOURNAL OF MEDICINAL CHEMISTRY

Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficacious in Vivo

(2013) Pravin S. Shirude et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis

(2013) Kevin Pethe et al.   NATURE MEDICINE

Identification of New Drug Targets and Resistance Mechanisms in Mycobacterium tuberculosis

(2013) Thomas R. Ioerger et al.   PLoS One

Novel inhibitors ofMycobacterium tuberculosisgrowth based on modified pyrimidine nucleosides and their analogues

(2013) E R Shmalenyuk et al.   RUSSIAN CHEMICAL REVIEWS

Mutations in panD encoding aspartate decarboxylase are associated with pyrazinamide resistance in Mycobacterium tuberculosis

(2013) Shuo Zhang et al.   Emerging Microbes & Infections

Synthesis and evaluation of 5′-modified thymidines and 5-hydroxymethyl-2′-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors

(2012) Kiran S. Toti et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Selective and Potent Inhibitors of Gram-Positive Bacterial Thymidylate Kinase (TMK)

(2012) Gabriel Martínez-Botella et al.   JOURNAL OF MEDICINAL CHEMISTRY

Delamanid for Multidrug-Resistant Pulmonary Tuberculosis

(2012) Maria Tarcela Gler et al.   NEW ENGLAND JOURNAL OF MEDICINE

Linezolid for Treatment of Chronic Extensively Drug-Resistant Tuberculosis

(2012) Myungsun Lee et al.   NEW ENGLAND JOURNAL OF MEDICINE

Para-Aminosalicylic Acid Acts as an Alternative Substrate of Folate Metabolism in Mycobacterium tuberculosis

(2012) S. Chakraborty et al.   SCIENCE

Mechanistic and structural basis for inhibition of thymidylate synthase ThyX

(2012) T. Basta et al.   Open Biology

Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase

(2011) Sara Van Poecke et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and Evaluation of 5-Substituted 2′-deoxyuridine Monophosphate Analogues As Inhibitors of Flavin-Dependent Thymidylate Synthase inMycobacterium tuberculosis

(2011) Martin Kögler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benzothiazinones Are Suicide Inhibitors of Mycobacterial Decaprenylphosphoryl-β-d-ribofuranose 2′-Oxidase DprE1

(2011) Claudia Trefzer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Decaprenylphosphoryl-β-D-Ribose 2′-Epimerase, the Target of Benzothiazinones and Dinitrobenzamides, Is an Essential Enzyme in Mycobacterium smegmatis

(2011) Paul K. Crellin et al.   PLoS One

Pyrazinamide Inhibits Trans-Translation in Mycobacterium tuberculosis

(2011) W. Shi et al.   SCIENCE

Fast Standardized Therapeutic-Efficacy Assay for Drug Discovery against Tuberculosis

(2010) J. Rullas et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines

(2010) Matthew L. Read et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Decaprenylphosphoryl-β-D-Ribose 2-Epimerase from Mycobacterium tuberculosis is a Magic Drug Target

(2010) G. Manina et al.   CURRENT MEDICINAL CHEMISTRY

Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone

(2010) Olga Familiar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and in vitro evaluation of antitubercular and antimicrobial activity of some novel pyranopyrimidines

(2010) Nimesh R. Kamdar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Benzothiazinones: Prodrugs That Covalently Modify the Decaprenylphosphoryl-β-d-ribose 2′-epimerase DprE1 ofMycobacterium tuberculosis

(2010) Claudia Trefzer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Arabinosyltransferase EmbC Is Inhibited by Ethambutol in Mycobacterium tuberculosis

(2009) R. Goude et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and antimycobacterial activity of 5-formylaminopyrimidines; analogs of antibacterial purines

(2009) Morten Brændvang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tuberculosis Treatment and Risk of Stavudine Substitution in First‐Line Antiretroviral Therapy

(2009) Daniel J. Westreich et al.   CLINICAL INFECTIOUS DISEASES

Design, synthesis and antimycobacterial activity of some novel imidazo[1,2-c]pyrimidines

(2009) Mahesh T. Chhabria et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

2-Substituted-4,5-Dihydroxypyrimidine-6-Carboxamide Antiviral Targeted Libraries

(2009) Vincent A. Boyd et al.   JOURNAL OF COMBINATORIAL CHEMISTRY

Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis

(2009) V. Makarov et al.   SCIENCE

High Content Screening Identifies Decaprenyl-Phosphoribose 2′ Epimerase as a Target for Intracellular Antimycobacterial Inhibitors

(2009) Thierry Christophe et al.   PLoS Pathogens

Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: Synthesis and in vitro anti-mycobacterial activity

(2008) Cécile Gasse et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure–activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-d-xylulose 5-phosphate synthase

(2008) Jialin Mao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Exploring Acyclic Nucleoside Analogues as Inhibitors ofMycobacterium tuberculosisThymidylate Kinase

(2008) Olga Familiar et al.   ChemMedChem

Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents

(2008) Moni Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Raltegravir: an integrase inhibitor for HIV-1

(2008) Teresa H Evering et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS