Synthesis and biological evaluation of novel 1, 2, 3-triazole derivatives as anti-tubercular agents. Issue 16 (15th August 2017)

• Record Type: Journal Article
• Authors: Aziz Ali, Abdul; Gogoi, Dhrubajyoti; Chaliha, Amrita K.; Buragohain, Alak K.; Trivedi, Priyanka; Saikia, Prakash J.; Gehlot, Praveen S.; Kumar, Arvind; Chaturvedi, Vinita; Sarma, Diganta
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 16(2017)
• Page Start: 3698
• Page End: 3703
• Publication Date: 2017-08-15
• Subjects: Tuberculosis -- 1, 2, 3-Triazoles -- Antimycobacterial activity -- Cytotoxicity -- Molecular docking; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.07.008
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A library of seventeen novel 1, 2, 3-triazole derivatives were efficiently synthesized in excellent yields by the popular 'click chemistry' approach and evaluated in vitro for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177 strain). Among the series, six compounds exhibited significant activity with minimum inhibitory concentration (MIC) values ranging from 3.12 to 0.78 μg/mL and along with no significant cytotoxicity against MBMDMQs (mouse bone marrow derived macrophages). Molecular docking of the target compounds into the active site of DprE1 (Decaprenylphosphoryl-β-d -ribose-2′-epimerase) enzyme revealed noteworthy information on the plausible binding interactions.