Article
Chemistry, Physical
Priyanka Yadav, C. P. Kaushik, Mukesh Kumar, Anil Kumar
Summary: A series of Phthalimide/Naphthalimide containing 1,2,3-triazole hybrids were synthesized through Click reaction. The compounds were characterized using various spectral techniques and the structure of compound 6b was confirmed by Single Crystal X-ray Crystallography. The synthesized hybrids showed excellent antimicrobial potency, particularly compound 6e, which demonstrated strong antimicrobial activity against all tested strains due to the presence of a nitro group on the phenyl ring. Molecular docking studies confirmed the binding conformation of compound 6e with E. coli topoisomerase II DNA gyrase B.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Reem I. Al-Wabli, Mona A. Alsulami, Sarah I. Bukhari, Nadine M. S. Moubayed, Maha S. Al-Mutairi, Mohamed I. Attia
Summary: A series of new indole-triazole conjugates were designed and synthesized for evaluation as new antimicrobial candidates, showing good to moderate activity against most tested Gram-negative strains and potent activity against Candida tropicalis, with one compound exhibiting the strongest activity against Candida albicans.
Article
Chemistry, Physical
Sana Saffour, Amal A. AL-Sharabi, Asaf Evrim Evren, Meral Yilmaz Cankilic, Leyla Yurttas
Summary: In this study, thirteen new compounds were synthesized and evaluated for their antifungal and antimicrobial activities. One compound exhibited the best activity and selectivity against Yersinia enterocolitica. Additionally, all compounds showed good activity against filamentous fungi.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Chemistry, Physical
Vineetha Telma D'Souza, Janardhana Nayak, Desmond Edward D'Mello, P. Dayananda
Summary: Triazoles and quinoline compounds have been well studied for their biological activities. In this study, a novel series of compounds were synthesized and screened for antimicrobial activities, with some showing significantly higher bioactivities compared to normal drugs.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Inorganic & Nuclear
Joel C. Mather, Jessica A. Wyllie, Alex Hamilton, Tatiana P. Soares da Costa, Peter J. Barnard
Summary: A series of gold(I) and silver(I) complexes were synthesized and their antibacterial activities were tested. The gold(I) complexes showed good activity against Gram-positive bacteria, with the complexes of the 1,2,4-triazolylidene ligands being more active. The silver(I) complexes exhibited good antibacterial activity against Acinetobacter baumannii. High levels of antibacterial activity were observed against multi-drug resistant bacterial strains for both the gold(I) and silver(I) complexes. Resistance to these metal-containing complexes was less likely to develop compared to the widely used broad-spectrum antibiotic. Furthermore, the stability of these complexes was investigated, revealing possible decomposition reactions for silver complexes in aqueous solution.
DALTON TRANSACTIONS
(2022)
Article
Pharmacology & Pharmacy
Mazen M. Almehmadi, Ahad M. Alsaiari, Mustafa Halawi, Osama Abdulaziz, Mohammad Asif
Summary: A series of novel ether compounds were synthesized and screened for antibacterial and antifungal activities. The compounds showed certain activity, but were less potent than standard drugs.
LATIN AMERICAN JOURNAL OF PHARMACY
(2022)
Article
Biochemistry & Molecular Biology
B. Sravanthi, G. Himavathi, A. R. Robert, Prashantha Karunakar, K. S. Kiran, S. Maddila
Summary: In this study, a new series of 1,3,4-oxadiazole and 1,2,4-triazole derivatives based on azaindole acetamides were synthesized and characterized as potential antibacterial and antitubercular substances. The structures of these compounds were determined by spectroscopic analysis. The compounds showed effective antibacterial and antifungal activities, particularly against S. aureus and A. flavus. Compounds 6e and 8b exhibited strong activity against M. tuberculosis. Molecular dynamics simulations and molecular docking revealed the potential biological activity of these compounds. The ADMET and physicochemical properties of the compounds were also evaluated.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Medicinal
Sampath Bitla, Akkiraju Anjini Gayatri, Muralidhar Reddy Puchakayala, Vijaya Kumar Bhukya, Jagadeshwar Vannada, Ramulu Dhanavath, Bhaskar Kuthati, Devender Kothula, Someswar Rao Sagurthi, Krisham Raju Atcha
Summary: A new series of bis-1,2,3- and 1,2,4-triazoles were designed and synthesized as potential antimicrobial agents, showing potent antimicrobial and promising antifungal activities. Compound 10f exhibited the best scores in molecular docking analysis, suggesting the introduction of para-chloro and bromo-phenyl aromatic groups could lead to excellent antimicrobial activity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Sobhi M. Gomha, Mastoura M. Edrees, Zeinab A. Muhammad, Nabila A. Kheder, Sraa Abu-Melha, Amirah M. Saad
Summary: In this study, many 1,4-dihydropyridines hybridized with 1,2,4-triazole were synthesized, yielding 1,4-dihydropyridine-bis-triazolothiadiazoles hybrid derivatives through cyclization. The chemical structure of the newly synthesized derivatives was characterized using elemental and spectral analysis. The results demonstrated that these derivatives exhibited better inhibitory activity against microorganisms.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Agriculture, Multidisciplinary
Muhan Ding, Suran Wan, Nan Wu, Ya Yan, Junhong Li, Xiaoping Bao
Summary: In this study, 52 novel compounds were designed, synthesized, and evaluated for their antimicrobial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Rhizoctonia solani. Some of these compounds showed excellent antibacterial activities and good pesticide-likeness, making them potential candidates for agricultural antimicrobial agents.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Polina O. Serebrennikova, Julia A. Paznikova, Eva A. Kirnos, Irina A. Utepova, Elizaveta D. Kazakova, Vladimir F. Lazarev, Liubov S. Kuznetcova, Boris A. Margulis, Irina V. Guzhova, Oleg N. Chupakhin, Alexey P. Sarapultsev
Summary: The present study synthesized new derivatives of mono- and bis-1,2,4-triazoloazines and evaluated their cytotoxic activity against cancer cells. These compounds exhibited significant toxicity towards tumor cells while having minimal effects on normal cells, suggesting their potential as effective and selective anticancer agents.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ping Yang, Jia-Bao Luo, Zi-Zhou Wang, Li-Lei Zhang, Jin Feng, Xiao-Bao Xie, Qing-Shan Shi, Xin-Guo Zhang
Summary: A series of 1,2,4-triazole-norfloxacin hybrids were designed, synthesized, and evaluated for their in vitro antibacterial activity against common pathogens. The newly synthesized compounds showed superior antibacterial activity to norfloxacin, with high toxicity towards bacterial cells but good biocompatibility. Molecular docking analysis suggested strong affinity of the compounds for bacterial topoisomerase IV.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Noha H. Amin, Mohamed T. El-Saadi, Ahmed A. Ibrahim, Hamdy M. Abdel-Rahman
Summary: Novel 5-amino-1,2,4-triazole derivatives and their cyclized 1,2,4-triazolo[1,5-a]pyrimidine analogues were designed, synthesized and evaluated for their antimicrobial activities. Compounds 9, 13a and 13b showed high to moderate antifungal activities against candida albicans, with considerable safety profiles, showing lower cytotoxicity against human embryonic kidney or red blood cells. Furthermore, compound 9 exhibited significant inhibitory activity against lansterol 14 alpha-demethylase compared to fluconazole, with favorable oral bioavailability predicted in in silico ADME studies.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Sara Sadeghian, Leila Emami, Ayyub Mojaddami, Soghra Khabnadideh, Zeinab Faghih, Kamyar Zomorodian, Maral Rashidi, Zahra Rezaei
Summary: Fungal infections pose a threat to human health due to drug resistance, highlighting the need for the design and development of novel antifungal agents. A series of 1,2,4-triazole derivatives were found to have potent antifungal activity, with compounds 7g and 7h showing enhanced activity against common and drug-resistant fungal strains. Molecular docking studies revealed their potential interaction with key enzyme active sites. These findings provide promising candidates for further clinical research.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Samet Poyraz, H. Ali Dondas, Jose M. Sansano, Samet Belveren, Cem Yamali, Mahmut Ulger, Naciye Yaktubay Dondas, Begum Nurpelin Saglik, Christopher M. Pask
Summary: A series of novel N-benzoylthiourea-pyrrolidine carboxylic acid derivatives with an imidazole moiety were synthesized and their various biological activities were evaluated. The molecules' ability to form intermolecular hydrogen bonds was studied to find the best antimicrobial activity. The compounds were tested for their enzyme inhibitory potency against AChE and BChE, which are the main targets for Alzheimer's disease. Additionally, the compounds were screened for antituberculosis and antibacterial activities, as well as antifungal activities against various strains of Candida.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)