Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, threats one-third of the world's population. Although numerous efforts have been undertaken to develop new anti-TB agents, only a handful of compounds have entered human trials in the past 5 decades. Triazoles including 1,2,3-triazole and 1,2,4-triazole are one of the most important classes of nitrogen containing heterocycles that exhibited various biological activities. Triazole derivatives are regarded as a new class of effective anti-TB candidates owing to their potential anti-TB potency. Thus, molecules containing triazole moiety may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistant to certain extent. This review outlines the advances in the application of triazole-containing hybrids as anti-TB agents, and discusses the structure-activity relationship of these derivatives.
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http://dx.doi.org/10.1016/j.ejmech.2017.06.051 | DOI Listing |
Sci Rep
December 2024
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Basic Medicine Research and Innovation Center for Novel Target and Therapeutic Intervention (Ministry of Education), Department of Urology and Department of Cancer Center of the Second Affiliated Hospital, College of Pharmacy, Chongqing Medical University, Chongqing, 400016, China. Electronic address:
Ferroptosis is a novel form of regulated cell death characterized by iron-dependent lipid ROS accumulation, which is associated with various diseases, including acute organ injury, neurodegenerative disorders, and cancer. Pharmacological inhibition of ferroptosis has great potential for the treatment of these diseases. However, the clinical translation of many ferroptosis inhibitors is hindered by their inadequate activity or suboptimal pharmacokinetic profiles.
View Article and Find Full Text PDFBioorg Chem
December 2024
Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran; Department of Persian Medicine, School of Medicine, Research Center for Traditional Medicine and History of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:
In the pursuit of developing potent α-glucosidase inhibitors for managing diabetes, a series of novel benzimidazole-acrylonitrile-1,2,3-triazole derivatives were designed. Sixteen derivatives (12a-p) were synthesized by varying substituents on the phenyl ring of the N-phenylacetamide moiety. Among these, compound 12m emerged as highly effective against α-glucosidase, displaying an IC value of 6.
View Article and Find Full Text PDFChem Biodivers
December 2024
Banaras Hindu University, Chemistry, institute of science, 221005, Varanasi, INDIA.
1,2,3-triazole-based ring connected with pyridazine, triazine, methyl pyrazole, diphenyl pyrazole, and pthalimide moieties through propylene linker have been synthesized for antidiabetic evaluation via click chemistry. The antidiabetic evaluations have been done by molecular docking studies and in- vitro tests and against the DPP-4 enzyme. The molecular docking studies have revealed that compounds 22, 23, 29, and 30 showed hydrogen bond with the DPP-4 enzyme while in vitro tests has revealed the compound 30 has (IC50 values 12.
View Article and Find Full Text PDFJ Biomol Struct Dyn
December 2024
Laboratory of Drug Design and Discovery, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Selective inhibition of histone deacetylase 8 (HDAC8) has emerged as a promising approach for treating various diseases, including cancer. However, finding key structural features for HDAC8 inhibition and developing effective and selective HDAC8 inhibitors (HDAC8s) pose significant challenges. In the past few years, the development of various scaffolds for inhibiting HDAC8 has significantly risen and the quest continues.
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