杂化和嵌合杂环对碳酸酐酶的抑制作用。

IF 4.8 3区 医学 Q2 CHEMISTRY, MEDICINAL
Pharmaceuticals Pub Date : 2025-09-16 DOI:10.3390/ph18091387
Niccolò Paoletti, Simone Giovannuzzi, Claudiu T Supuran
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引用次数: 0

摘要

设计多靶点药物是解决复杂和多因素疾病的一种日益增长的策略,杂环化合物在这一方法中起着重要作用。本文旨在批判性地分析杂环支架在人类碳酸酐酶抑制剂(hCAIs)开发中的作用,强调其作为核心化学型、连接体和次级药物载体的多功能性。通过研究过去10年的进展,我们强调了基于杂环的设计如何有助于调节对hCAs的效力和选择性,以及创造具有增强治疗概况的杂交分子。了解这些策略对于指导未来针对hCAs和相关病理的药物发现工作至关重要。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Hybrid and Chimeric Heterocycles for the Inhibition of Carbonic Anhydrases.

The design of multitarget drugs is a growing strategy to address complex and multifactorial diseases, and heterocycles play a major role in this approach. This review aims to critically analyze the role of heterocyclic scaffolds in the development of human carbonic anhydrase inhibitors (hCAIs), emphasizing their versatility as core chemotypes, linkers, and secondary pharmacophores. By examining advances from the last 10 years, we highlight how heterocycle-based designs contribute to modulating potency and selectivity toward hCAs, as well as to the creation of hybrid molecules with enhanced therapeutic profiles. Understanding these strategies is essential for guiding future drug discovery efforts targeting hCAs and related pathologies.

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来源期刊
Pharmaceuticals
Pharmaceuticals Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.10
自引率
4.30%
发文量
1332
审稿时长
6 weeks
期刊介绍: Pharmaceuticals (ISSN 1424-8247) is an international scientific journal of medicinal chemistry and related drug sciences.Our aim is to publish updated reviews as well as research articles with comprehensive theoretical and experimental details. Short communications are also accepted; therefore, there is no restriction on the maximum length of the papers.
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