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吲哚-三唑分子杂合体:药物发现的前沿领域述评:现状与未来展望。

A Review on Indole-triazole Molecular Hybrids as a Leading Edge in Drug Discovery: Current Landscape and Future Perspectives.

机构信息

Department of Pharmaceutical Chemistry, SGT College of Pharmacy, Shree Guru Gobind Singh Tricentenary University, Gurugram, Haryana, India.

出版信息

Curr Top Med Chem. 2024;24(18):1557-1588. doi: 10.2174/0115680266307132240509065351.

Abstract

Molecular hybridization is a rational design strategy used to create new ligands or prototypes by identifying and combining specific pharmacophoric subunits from the molecular structures of two or more known bioactive derivatives. Molecular hybridization is a valuable technique in drug discovery, enabling the modulation of unwanted side effects and the creation of potential dual-acting drugs that combine the effects of multiple therapeutic agents. Indole-triazole conjugates have emerged as promising candidates for new drug development. The indole and triazole moieties can be linked through various synthetic strategies, such as click chemistry or other coupling reactions, to generate a library of diverse compounds for biological screening. The achievable structural diversity with indole-triazole conjugates offers avenues to optimize their pharmacokinetic and pharmacodynamic attributes, amplifying their therapeutic efficacy. Researchers have extensively tailored both indole and triazole frameworks with diverse modifications to comprehend their impact on the drug's pharmacokinetic and pharmacodynamic characteristics. The current review article endeavours to explore and discuss various research strategies to design indoletriazole hybrids and elucidate their significance in a variety of pathological conditions. The insights provided herein are anticipated to be beneficial for the researchers and will likely encourage further exploration in this field.

摘要

分子杂交是一种合理的设计策略,通过识别和组合两个或多个已知生物活性衍生物的分子结构中的特定药效基团,来创建新的配体或原型。分子杂交是药物发现中的一项有价值的技术,能够调节不必要的副作用,并创造潜在的双重作用药物,将多种治疗剂的效果结合在一起。吲哚-三唑缀合物已成为新药开发的有前途的候选物。吲哚和三唑部分可以通过各种合成策略(如点击化学或其他偶联反应)连接,生成用于生物筛选的多样化化合物库。通过吲哚-三唑缀合物实现的结构多样性为优化其药代动力学和药效学特性提供了途径,增强了其治疗效果。研究人员已经广泛地对吲哚和三唑框架进行了各种修饰,以了解它们对药物药代动力学和药效学特征的影响。本文综述文章旨在探讨和讨论设计吲哚-三唑杂合体的各种研究策略,并阐明它们在各种病理条件下的意义。预计本文提供的见解将对研究人员有益,并可能鼓励该领域的进一步探索。

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