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恶二唑:药物发现中极具多功能性的支架。

Oxadiazole: A highly versatile scaffold in drug discovery.

机构信息

Division of Medicinal Chemistry, Department of Chemistry, Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar, Gujarat, India.

School of Pharmacy, Vishwakarma University, Pune, Maharashtra, India.

出版信息

Arch Pharm (Weinheim). 2022 Sep;355(9):e2200123. doi: 10.1002/ardp.202200123. Epub 2022 May 16.

DOI:10.1002/ardp.202200123
PMID:35575467
Abstract

As a pharmacologically important heterocycle, oxadiazole paved the way to combat the problem associated with the confluence of many commercially available drugs with different pharmacological profiles. The present review focuses on the potential applications of five-membered heterocyclic oxadiazole derivatives, especially 1,2,4-oxadiazole, 1,2,5-oxadiazole, and 1,3,4-oxadiazole, as therapeutic agents. Designing new hybrid molecules containing the oxadiazole moiety is a better solution for the development of new drug molecules. The designed molecules may accumulate a biological profile better than those of the drugs currently available on the market. The present review will guide the way for researchers in the field of medicinal chemistry to design new biologically active molecules based on the oxadiazole nucleus. Antitubercular, antimalarial, anti-inflammatory, anti-HIV, antibacterial, and anticancer activities of various oxadiazoles have been reviewed extensively here.

摘要

作为一种具有重要药理学意义的杂环,恶二唑为解决许多具有不同药理学特性的市售药物融合所带来的问题铺平了道路。本综述重点介绍了五元杂环恶二唑衍生物(特别是 1,2,4-恶二唑、1,2,5-恶二唑和 1,3,4-恶二唑)作为治疗剂的潜在应用。设计含有恶二唑部分的新型杂分子是开发新药物分子的更好解决方案。与市场上现有的药物相比,设计的分子可能会更好地积累生物学特征。本综述将为药物化学领域的研究人员提供指导,以基于恶二唑核设计新的具有生物活性的分子。本文广泛综述了各种恶二唑的抗结核、抗疟、抗炎、抗 HIV、抗菌和抗癌活性。

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