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

被引:38
作者
Reddy, Dinesh S. [1 ]
Hosamani, Kallappa M. [1 ]
Devarajegowda, Hirihalli C. [2 ]
Kurjogi, Mahantesh M. [3 ]
机构
[1] Karnatak Univ, PG Dept Studies Chem, Dharwad 580003, Karnataka, India
[2] Univ Mysore, Yuvarajas Coll, Dept Phys, Mysore 570005, Karnataka, India
[3] Karnatak Univ, PG Dept Studies Microbiol & Biotechnol, Dharwad 580003, Karnataka, India
关键词
BACTERIAL PROTEIN-SYNTHESIS; IN-VITRO; ANTIMYCOBACTERIAL CONSTITUENTS; MYCOBACTERIUM-TUBERCULOSIS; BIOLOGICAL EVALUATION; DIALLYL SULFIDE; ANTICANCER; ANTIOXIDANT; INHIBITION; CHEMISTRY;
D O I
10.1039/c5ra09508e
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:64566 / 64581
页数:16
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