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  3. Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents

Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents

  • Bioorg Med Chem Lett. 2017 Aug 15;27(16):3698-3703. doi: 10.1016/j.bmcl.2017.07.008.
Abdul Aziz Ali 1,  Dhrubajyoti Gogoi 2,  Amrita K Chaliha 2,  Alak K Buragohain 2,  Priyanka Trivedi 3,  Prakash J Saikia 4,  Praveen S Gehlot 5,  Arvind Kumar 5,  Vinita Chaturvedi 6,  Diganta Sarma 7
Affiliations

Affiliations

  • 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.
  • 6 Biochemistry Division, Central Drug Research Institute, CSIR, Lucknow 226001, India. Electronic address: vinita_chaturvedi@cdri.res.in.
  • 7 Department of Chemistry, Dibrugarh University, Dibrugarh 786004, Assam, India. Electronic address: dsarma22@gmail.com.
PMID: 28712709 DOI: 10.1016/j.bmcl.2017.07.008
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 0.78μg/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.

Keywords

1,2,3-Triazoles; Antimycobacterial activity; Cytotoxicity; Molecular docking; Tuberculosis.

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