推进药物发现:作为药物化学和药理学多面手的噻二唑衍生物

IF 3.3 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Bioorganic & Medicinal Chemistry Pub Date : 2024-08-16 DOI:10.1016/j.bmc.2024.117876
Benjamin Ayodipupo Babalola , Lekhnath Sharma , Olanike Olowokere , Monika Malik , Oreoluwa Folajimi
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引用次数: 0

摘要

在科学技术飞速发展的今天,人们正努力遏制与健康有关的疾病。研究发现凸显了杂环化合物,尤其是噻二唑衍生物的价值,因为它们具有多种药理活性。这些化合物在治疗医学和开发有效药物方面发挥着至关重要的作用。噻二唑是由一个硫原子和两个氮原子组成的五元杂环化合物。本综述探讨了先进的合成技术,包括使用异质催化剂、微波辅助方法、超声辅助合成、无溶剂工艺、多组分反应、铜催化的有氧氧化环化、分子内环化、点击化学支持合成以及碱促进的无过渡金属介导合成。这些方法增强了噻二唑化合物的多样性和潜在应用。此外,本研究还提供了有关噻二唑衍生物关键药理活性的最新信息,凸显了它们在治疗药物开发方面的潜力。研究还讨论了结构-活性关系(SAR),以便更好地了解它们在生物系统中的相互作用和安全性。这项工作旨在扩展已报道的噻二唑分子的化学性质和药理潜力,以验证其作为药物设计和开发中具有前景的药层的功效。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Advancing drug discovery: Thiadiazole derivatives as multifaceted agents in medicinal chemistry and pharmacology

In this dispensation of rapid scientific and technological advancements, significant efforts are being made to curb health-related diseases. Research discoveries have highlighted the value of heterocyclic compounds, particularly thiadiazole derivatives, due to their diverse pharmacological activities. These compounds play a crucial role in therapeutic medicine and the development of effective drugs. Thiadiazoles are five-membered heterocyclic compounds consisting of one sulfur and two nitrogen atoms. This review explores advanced synthesis techniques, including the use of heterogeneous catalysts, microwave-assisted methods, ultrasound-assisted synthesis, solvent-free processes, multicomponent reactions, copper-catalyzed aerobic oxidative annulation, intramolecular cyclization, click-chemistry supported synthesis, and alkali-promoted, transition-metal-free mediated synthesis. These methods enhance the diversity and potential applications of thiadiazole compounds. Furthermore, this study provides up-to-date information on the key pharmacological activities of thiadiazole derivatives, highlighting their potential in therapeutic medicine for drug development. The structure–activity relationship (SAR) is also discussed to better understand their interactions and safety in biological systems. This work aims to expand on the reported chemistry and pharmacological potential of the thiadiazole moiety to validate their efficacy as promising pharmacophores in drug design and development.

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来源期刊
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry 医学-生化与分子生物学
CiteScore
6.80
自引率
2.90%
发文量
413
审稿时长
17 days
期刊介绍: Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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