TITLE:
Novel 1,3,4-(thiadiazol-2-ylamino) methyl-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-thiones: synthesis, docking and antimycobacterial testing
AUTHORS:
Trupti S. Chitre, Santosh Panda, Shital M Patil, Aparna S. Chothe, G Vignesh, M. K. Kathiravan
KEYWORDS:
Mannich Base; Oxadiazole; Thiadiazole; Antimycobacterial; Docking
JOURNAL NAME:
Advances in Biological Chemistry,
Vol.1 No.2,
August
22,
2011
ABSTRACT: In the present study, a novel series of Mannich bases of 3-substituted 5-(pyridin-4-yl)-1,3, 4-oxadiazol-2-thione derivatives were synthesized. Docking study was performed to rationalize the possible interactions between the synthesized com-pounds and active site of 14DM. The test compounds were screened for antimycobacterial activity using Middlebrook 7H9 medium against M. tuberculosis H37Rv (ATCC 27294) as well as Isoniazid (INH) resistant clinical strain. Among the series 5c and 5a are found to be most potent (susceptible) while the compound 5f did not show activity against M. tuberculosis H37Rv (resistant). The SAR study reveals the importance of substitutions at para position for good activity.