Open AccessSYNTHESIS OF INDOLE, COUMARINYL AND PYRIDINYL DERIVATIVES OF ISONIAZID AS POTENT ANTITUBERCULAR AND ANTIMICROBIAL AGENTS AND THEIR MOLECULAR DOCKING STUDIES
Author(s) -
A. S. Rathod,
Shivakumar S. Godipurge,
J. S. Biradar
Publication year - 2017
Publication title -
international journal of pharmacy and pharmaceutical sciences/international journal of pharmacy and pharmaceutical sciences
Language(s) - English
Resource type - Journals
eISSN - 2656-0097
pISSN - 0975-1491
DOI - 10.22159/ijpps.2017v9i12.21970
Subject(s) - antimicrobial , isoniazid , chemistry , antioxidant , indole test , docking (animal) , combinatorial chemistry , mode of action , stereochemistry , biochemistry , tuberculosis , organic chemistry , medicine , nursing , pathology
Objective: The aim of this study was to the synthesis of indole, coumarinyl and pyridinyl derivatives of isoniazid as potent anti-TB and antimicrobial agents and their molecular docking studies.Methods: The structures of the newly synthesized compounds were confirmed by FT-IR, 1HNMR, and Mass spectroscopic methods and to evaluate the biological studies like anti-TB, antimicrobial and antioxidant activities. The mode of action of these active compounds was carried out by molecular docking studies.Results: Among all the synthesized compounds tested 5d was found to be the most active with M. tuberculosis H37Rv strain at 12.5µg/ml, 5b at 25µg/ml, 4d was found to be the most active with S. typhi, S. aureus and A. Nizer, 5a with A. Oryzae, 5c with A. terrous and A. Flavous and 5d with Shegella at 100µg/ml and some of the compounds like 4d, 5a, 5b and 5d have shown promising antioxidant properties.Conclusion: All the synthesized compounds have exhibited promising anti-TB, antimicrobial and antioxidant activities.