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Click chemistry based regioselective one‐pot synthesis of coumarin‐3‐yl‐methyl‐1,2,3‐triazolyl‐1,2,4‐triazol‐3(4 H )‐ones as newer potent antitubercular agents
Author(s) -
Somagond Shilpa M.,
Kamble Ravindra R.,
Bayannavar Praveen K.,
Shaikh Saba Kauser J.,
Joshi Shrinivas D.,
Kumbar Vijay M.,
Nesaragi Aravind R.,
Kariduraganavar Mahadevappa Y.
Publication year - 2019
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201900013
Subject(s) - coumarin , chemistry , click chemistry , cycloaddition , docking (animal) , triazole , autodock , cytotoxicity , stereochemistry , 1,2,3 triazole , inha , combinatorial chemistry , mtt assay , regioselectivity , mycobacterium tuberculosis , in vitro , biochemistry , organic chemistry , catalysis , tuberculosis , in silico , gene , medicine , nursing , pathology
Coumarin‐3‐yl‐methyl‐1,2,3‐triazolyl‐1,2,4‐triazol‐3(4 H )‐ones ( 8k‐z ) were synthesized via copper(I)‐catalyzed azide‐alkyne cycloaddition click chemistry. The synthesized hybrid molecules were characterized by spectral studies. Compounds 8k‐z were screened for their in vitro anti‐TB activity by using the Microplate Alamar Blue assay and for cytotoxicity using the MTT assay. Some of the compounds were found to be most potent against the tested Mycobacterium tuberculosis H37Rv strain with a MIC of 1.60 µg/ml. Further, docking the compounds into the InhA binding pocket showed strong binding interactions and effective overall docking scores were recorded. The drug‐likeness and toxicity studies were computed using Molinspiration and Protox, respectively.