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抗结核药物。第 6 部分:新型芳基磺酰胺基偶联恶唑烷酮的合成及抗分枝杆菌活性。

Anti-tubercular agents. Part 6: synthesis and antimycobacterial activity of novel arylsulfonamido conjugated oxazolidinones.

机构信息

Division of Organic Chemistry-I, Indian Institute of Chemical Technology, Hyderabad 500 607, India.

出版信息

Eur J Med Chem. 2011 Mar;46(3):893-900. doi: 10.1016/j.ejmech.2010.12.028. Epub 2011 Jan 9.

Abstract

As a part of investigation of new anti-tubercular agents in this laboratory, herein we describe the synthesis of a new class of arylsulfonamido conjugated oxazolidinones. The in vitro activity of these conjugated (6a-f, 7a-d, 9a-c and 11a-c) molecules against Mycobacterium tuberculosis H(37)Rv by using rifampicin and linezolide as positive controls is discussed, compounds 7c and 9a-c are found to be the most active members in this series. Further, cytotoxicity of the potent conjugates of the series (7c, and 9a-c) was evaluated on human foreskin fibroblast (HFF) cells by using MTT assay. Finally, these studies suggest that compounds 7c and 9a may serve as promising lead scaffolds for further generation of new as anti-TB agents.

摘要

作为本实验室研究新型抗结核药物的一部分,本文描述了一类新型芳基磺酰胺偶联恶唑烷酮的合成。通过使用利福平利福平和利奈唑胺作为阳性对照,讨论了这些共轭(6a-f、7a-d、9a-c 和 11a-c)分子对结核分枝杆菌 H(37)Rv 的体外活性,发现化合物 7c 和 9a-c 是该系列中最有效的成员。此外,通过 MTT 测定法评估了该系列中具有潜在细胞毒性的共轭物(7c 和 9a-c)对人包皮成纤维细胞(HFF)的细胞毒性。最后,这些研究表明,化合物 7c 和 9a 可能作为有前途的新型抗结核药物的先导骨架。

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