Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents |
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| Authors: | Abdul Aziz Ali Dhrubajyoti Gogoi Amrita K Chaliha Alak K Buragohain Priyanka Trivedi Prakash J Saikia Praveen S Gehlot Arvind Kumar Vinita Chaturvedi Diganta Sarma |
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| Institution: | 1. Department of Chemistry, Dibrugarh University, Dibrugarh 786004, Assam, India;2. DBT-Bioinformatics Infrastructure Facility, Centre for Biotechnology and Bioinformatics, Dibrugarh University, Dibrugarh 786004, Assam, India;3. Biochemistry Division, Central Drug Research Institute, CSIR, Lucknow 226001, India;4. Analytical Chemistry Division, CSIR-North East Institute of Science & Technology, Jorhat 785006, Assam, India;5. AcSIR, Salt and Marine Chemicals Division, CSIR-Central Salt and Marine Chemicals Research Institute, Bhavnagar 364002, India |
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| 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. |
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| Keywords: | Tuberculosis 1 2 3-Triazoles Antimycobacterial activity Cytotoxicity Molecular docking |
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