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拓展喹喔啉-7-羧酸酯1,4-二氧化物衍生物作为潜在抗结核药物的化学空间。

Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di--oxide derivatives as potential antitubercular agents.

作者信息

González-González Alonzo, Sánchez-Sánchez Oscar, Wan Baojie, Franzblau Scott, Palos Isidro, Espinoza-Hicks José C, Moreno-Rodríguez Adriana, Martínez-Vázquez Ana Verónica, Lara-Ramírez Edgar E, Ortiz-Pérez Eyra, Paz-González Alma D, Rivera Gildardo

机构信息

Laboratorio de Biotecnología Farmacéutica, Centro de Biotecnología Genómica, Instituto Politécnico Nacional Mexico

Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago USA.

出版信息

RSC Med Chem. 2024 Jul 17;15(8):2785-2791. doi: 10.1039/d4md00221k. eCollection 2024 Aug 14.

Abstract

Tuberculosis is a worldwide health problem that warrants attention given that the current treatment options require a long-term chemotherapeutic period and have reported the development of () multidrug resistant strains. In this study, -butyl and isobutyl quinoxaline-7-carboxylate 1,4-di--oxide were evaluated against replicating and non-replicating H37Rv strains. The results showed that seventeen of the twenty-eight derivatives have minimum inhibitory concentration (MIC) values lower than isoniazid (2.92 μM). The most active antimycobacterial agents were , , , and , which have the lowest MIC values (0.53, 0.57, 0.53, and 0.55 μM respectively). These results confirm the potential of quinoxaline-1,4-di--oxide against to develop and obtain new and more safety antituberculosis drugs.

摘要

结核病是一个全球性的健康问题,鉴于目前的治疗方案需要长期化疗,并且已报道出现了()多重耐药菌株,因此值得关注。在本研究中,对丁基和异丁基喹喔啉 -7- 羧酸 1,4- 二氧化物针对增殖型和非增殖型 H37Rv 菌株进行了评估。结果表明,28 种衍生物中的 17 种的最低抑菌浓度(MIC)值低于异烟肼(2.92 μM)。活性最强的抗分枝杆菌剂是 、 、 和 ,它们具有最低的 MIC 值(分别为 0.53、0.57、0.53 和 0.55 μM)。这些结果证实了喹喔啉 -1,4- 二氧化物在开发和获得新型、更安全的抗结核药物方面针对 的潜力。

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