| Literature DB >> 28712709 |
Abdul Aziz Ali1, Dhrubajyoti Gogoi2, Amrita K Chaliha2, Alak K Buragohain2, Priyanka Trivedi3, Prakash J Saikia4, Praveen S Gehlot5, Arvind Kumar5, Vinita Chaturvedi6, Diganta Sarma7.
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.Entities:
Keywords: 1,2,3-Triazoles; Antimycobacterial activity; Cytotoxicity; Molecular docking; Tuberculosis
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Year: 2017 PMID: 28712709 DOI: 10.1016/j.bmcl.2017.07.008
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823