Advances in Biological Chemistry

Volume 1, Issue 2 (August 2011)

ISSN Print: 2162-2183   ISSN Online: 2162-2191

Google-based Impact Factor: 0.5  Citations  

Novel 1,3,4-(thiadiazol-2-ylamino) methyl-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-thiones: synthesis, docking and antimycobacterial testing

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DOI: 10.4236/abc.2011.12002    7,379 Downloads   19,337 Views  Citations

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.

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Chitre, T. , Panda, S. , Patil, S. , Chothe, A. , Vignesh, G. and Kathiravan, M. (2011) Novel 1,3,4-(thiadiazol-2-ylamino) methyl-5-(pyridin-4-yl)-1,3,4-oxadiazol-2-thiones: synthesis, docking and antimycobacterial testing. Advances in Biological Chemistry, 1, 7-14. doi: 10.4236/abc.2011.12002.

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