| Literature DB >> 25765907 |
Naveen Polkam1, Parsharamulu Rayam1, Jaya Shree Anireddy2, Satyanarayana Yennam3, Hasitha Shilpa Anantaraju4, Sriram Dharmarajan4, Yogeeswari Perumal4, Sudha Sravanti Kotapalli5, Ramesh Ummanni5, Sridhar Balasubramanian6.
Abstract
A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives 5a-5l, 7a-7e and 9 have been synthesised and screened for in vitro antimycobacterial activity against Mycobacterium smegmatis MC-155. In addition these compounds have also been screened for cytotoxic activity against cancer cell lines HT-29, MDA-MB-231 by MTT colorimetric assay. The compounds are well characterized by spectral analysis viz. (1)H NMR, (13)C NMR, FT-IR, mass and HRMS. Screening results indicate that compounds 5g, 7a possess good antitubercular activity with MIC value 65.74 and 40.86, respectively, compounds 5g, 7a, 7b, 7d, 7e and 9 displayed promising cytotoxic activity against the cell lines tested. 5g and 7a stand out to be potent antimycobacterial and anticancer agents among the tested series. Further the title compounds were also tested on human normal cells HEK293T and are found to be safer with lesser cytotoxicity. It is interesting to observe that compound 5g has come out to be safer, potent anticancer and antimycobacterial agent.Entities:
Keywords: 2,5-Disubstitued-1,3,4-thiadiazole; Anti-mycobacterial activity; Cytotoxic activity; In vitro studies; MTT colorimetric assay
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Year: 2015 PMID: 25765907 DOI: 10.1016/j.bmcl.2015.02.052
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823