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首页> 外文期刊>RSC Advances >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
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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

机译：基于新生物分子的香豆素 - 噻唑啉杂交物作为具有细胞毒性，DNA裂解和X射线研究的有效抗结核剂的容易合成与评价。

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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.
机译：在微波辐射下的高效和快速合成香豆素 - 噻唑啉杂交物（1A-1J），具有高收率。使用元素和光谱分析表征合成化合物;另外，使用单晶X射线衍射技术阐明化合物1a，1b，1e和1h的结构。将所有新合成的化合物筛选在体外抗结核活动和DNA切割研究中，而最活跃的化合物在VERO细胞系上进行细胞毒性测定。在那些测试的那些中，化合物1b具有具有低水平的细胞毒性的优异的抗结核活性（MIC 0.09mg ml（-1）），表明化合物1b是用于寻找新的抗结核剂的后续调查的有前途的铅。此外，使用琼脂糖凝胶电泳方法的DNA切割研究显示，化合物1b，1d，1f和1i更有效地切割DNA，从而表现出核酸酶活性。

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