吲哚-噻唑杂化支架的最新进展:合成、分子杂交和药理潜力。

IF 3.8 3区 医学 Q2 PHARMACOLOGY & PHARMACY
Doaa A Abdelrheem, Sally Mostafa Khadrawy, Mohamed A M Ali, Saleh Alkhedhairi, Faris F Aba Alkhayl, Al Mokhtar Lamsabhi, Emadeldin M Kamel
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引用次数: 0

摘要

近年来,吲哚-噻唑杂化物在药物化学领域引起了越来越多的兴趣,它们将吲哚核与噻唑环结合在一个单一的框架内。吲哚单元为π-π相互作用和氢键提供了机会,而噻唑环可以调节亲脂性和电子性质,并可以支持额外的杂原子介导的相互作用。本文综述了吲哚-噻唑类化合物的合成方法、构效关系、计算研究和已报道的生物活性。讨论的应用包括抗癌和抗菌研究,抗糖尿病活性和选定的酶抑制。强调了绿色多组分路线、基于结构的设计和对接以及ADMET(吸收、分布、代谢、排泄和毒性)评估等新兴方向。最后,本文概述了优化吲哚-噻唑复合物作为治疗先导的主要挑战和前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Recent advances in indole-thiazole hybrid scaffolds: synthesis, molecular hybridization, and pharmacological potential.

Indole-thiazole hybrids have attracted increasing interest in medicinal chemistry in recent years, combining the privileged indole nucleus with the thiazole ring within a single framework. The indole unit offers opportunities for π-π interactions and hydrogen bonding, while the thiazole ring enables tuning of lipophilicity and electronic properties and can support additional heteroatom-mediated interactions. This review summarizes synthetic approaches, structure-activity relationships (SAR), computational studies, and reported biological activities of indole-thiazole hybrids. The discussed applications include anticancer and antimicrobial studies, antidiabetic activity, and selected enzyme inhibition. Emerging directions such as greener multicomponent routes, structure-based design and docking, and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) evaluation are highlighted. Finally, key challenges and perspectives for optimizing indole-thiazole hybrids as therapeutic leads are outlined.

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来源期刊
Pharmacological Reports
Pharmacological Reports 医学-药学
CiteScore
8.40
自引率
0.00%
发文量
91
审稿时长
6 months
期刊介绍: Pharmacological Reports publishes articles concerning all aspects of pharmacology, dealing with the action of drugs at a cellular and molecular level, and papers on the relationship between molecular structure and biological activity as well as reports on compounds with well-defined chemical structures. Pharmacological Reports is an open forum to disseminate recent developments in: pharmacology, behavioural brain research, evidence-based complementary biochemical pharmacology, medicinal chemistry and biochemistry, drug discovery, neuro-psychopharmacology and biological psychiatry, neuroscience and neuropharmacology, cellular and molecular neuroscience, molecular biology, cell biology, toxicology. Studies of plant extracts are not suitable for Pharmacological Reports.
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