A facile synthesis and evaluation of new biomolecule-based coumarin-thiazoline hybrids as potent anti-tubercular agents with cytotoxicity, DNA cleavage and X-ray studies

Reddy, D. S. and Hosamani, K. M. and Devarajegowda, H. C. and Kurjogi, M. M. (2015) A facile synthesis and evaluation of new biomolecule-based coumarin-thiazoline hybrids as potent anti-tubercular agents with cytotoxicity, DNA cleavage and X-ray studies. RSC ADVANCES, 5 (79). pp. 64566-64581. ISSN 2046-2069

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Official URL: http://doi.org/10.1039/c5ra09508e

Abstract

An efficient and rapid synthesis of coumarin-thiazoline hybrids (1a-1j) under microwave irradiation is described with high yields. The synthesized compounds were characterized using elemental and spectroscopic analysis; in addition, the structures of compounds 1a, 1b, 1e and 1h have been elucidated using single crystal X-ray diffraction techniques. All the newly synthesized compounds were screened for their in vitro anti-tubercular activity and in a DNA cleavage study, while the most active compounds were subjected to a cytotoxicity assay on Vero cell lines. Among those tested, compound 1b exhibited excellent anti-tubercular activity (MIC 0.09 mg ml(-1)) with a low level of cytotoxicity, suggesting that compound 1b is a promising lead for subsequent investigations in search of new anti-tubercular agents. Furthermore, a DNA cleavage study using an agarose gel electrophoresis method revealed that compounds 1b, 1d, 1f and 1i cleaved DNA more efficiently and thereby exhibit nuclease activity.

Item Type: Article
Subjects: D Physical Science > Physics
Divisions: Yuvaraj college > Physics
Depositing User: Shrirekha N
Date Deposited: 18 Jun 2019 05:45
Last Modified: 18 Jun 2019 05:45
URI: http://eprints.uni-mysore.ac.in/id/eprint/3251

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