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靛红杂合体及其药理学研究。

Isatin Hybrids and Their Pharmacological Investigations.

机构信息

Department of Pharmaceutical Chemistry, DKSS's Institute of Pharmaceutical Science and Research, Swami Chincholi, Dist-Pune, 413130 Maharashtra, India.

PES's Modern College of Pharmacy, Nigdi, Pune, 411044, Maharashtra, India.

出版信息

Mini Rev Med Chem. 2021;21(10):1182-1225. doi: 10.2174/1389557520999201209213029.

DOI:10.2174/1389557520999201209213029
PMID:33302835
Abstract

Hybridization is an important strategy to design molecules that can be effectively used to treat fatal diseases known to mankind. Molecular hybrids and their pharmacological investigations aided in discovering several potent isatin (Indole 2, 3 dione) derivatives with anti-HIV, antimalarial, antitubercular, antibacterial, and anticancer activities. Indole-2,3-dione and their derivatives have diverse pharmacological properties and have a prominent role in the discovery of new drugs. To understand the various approaches for designing new molecules based on isatin nucleus analysis of various pharmacophore hybrids, spacers/linkers between pharmacophores and isatin for hybridization and their biological activities are important. This review discusses the progress in developing isatin hybrids as biologically effective agents and their crucial aspects of design and structure-activity relationships.

摘要

杂交是设计能够有效治疗人类已知致命疾病的分子的重要策略。分子杂种及其药理学研究有助于发现几种具有抗 HIV、抗疟疾、抗结核、抗菌和抗癌活性的有效的靛红(吲哚 2,3-二酮)衍生物。吲哚-2,3-二酮及其衍生物具有多种药理学特性,在新药发现中起着重要作用。为了了解基于靛红核的各种药理学杂合分子的设计方法,研究了杂合分子中各种药效团之间的间隔物/连接物、药效团与靛红之间的杂交以及它们的生物活性。本文综述了将靛红杂合作为生物有效剂的发展进展及其设计和构效关系的关键方面。

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