4.4 Article

Click Chemistry Inspired Design, Synthesis and Molecular Docking Studies of Coumarin, Quinolinone Linked 1,2,3-Triazoles as Promising Anti-Microbial Agents

Journal

CHEMISTRYSELECT
Volume 3, Issue 19, Pages 5296-5303

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201800319

Keywords

Anti-microbial; Click Chemistry; Coumarin; Molecular Modeling Study; Quinolinone; Structural-activity Relationship (SAR) Studies; Triazoles

Funding

  1. Department of Science and Technology, Science and Engineering Research Board New Delhi (DST-SERB) Project [SB/FT/CS-175/2013]

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A series of new coumarin, quinolinone and benzyl linked 1,2,3-triazole derivatives have been synthesized and screened for their anti-bacterial and anti-fungal activities. Results of bioassay indicate that, compounds containing chloro and methoxy substituents in coumarin (6j), chloro substitution in quinolinone (7g) and 3-chloro benzyl analogue (8f) exhibit excellent anti-bacterial activities. The results of anti-fungal activities also reveal that methoxy and chloro substituted coumarins (6e and 6j) were highly active against yeast strains, in addition, chloro and methyl substituted coumarins (6h and 6i) were also exhibited excellent activity. Further, methyl substituted quinolinone with chloro substituted coumarin (7f) was found to highly active against yeast fungi and filamentous strain A.niger. It is evident from the results obtained and SAR studies that electron withdrawing or donating character of the substituents do not seem to be a major factor in increasing or decreasing anti-microbial activity.

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