共享氨基甲酸酯支架的内源性大麻素降解酶的有望抑制剂。

IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Mini reviews in medicinal chemistry Pub Date : 2024-11-25 DOI:10.2174/0113895575328120241107061303
Shivani Jaiswal, Senthil Raja Ayyannan
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引用次数: 0

摘要

氨基甲酸酯在近代药物发现中被广泛用作支架,也是许多已批准药物的常见结构基团。氨基甲酸酯分子独特的酰胺酯杂化(-O-CO-NH-)特征为设计特定的药物-靶点相互作用提供了可能。尽管发现了许多作用于内源性大麻素系统(ECS)的氨基甲酸酯衍生物,但开发临床有效的氨基甲酸酯药物仍是一项挑战。在这篇综述中,我们强调了氨基甲酸酯类内源性大麻素降解酶抑制剂的治疗潜力,认为这是发现神经治疗药物的一个突破口。我们讨论了通过干扰脂肪酸酰胺水解酶(FAAH)、单酰甘油脂肪酶(MAGL)和含α/β-水解酶结构域的6(ABHD6)来调节内源性大麻素信号通路的氨基甲酸酯类分子结构的设计策略和药物化学方面的问题。此外,我们还强调了氨基甲酸酯类药物对 FAAH 和 MAGL、FAAH 和胆碱酯酶以及 FAAH 和 TRPV1 通道的双重活性特征。此外,我们还说明了 O-官能化氨基甲酸酯和 N-环氨基甲酸酯的药理作用,它们分别对 FAAH 和 MAGL 的抑制活性至关重要。
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Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold.

Carbamate has been extensively used as a scaffold in the recent era of drug discovery and is a common structural motif of many approved drugs. The carbamate moiety's unique amide-ester hybrid (-O-CO-NH-) feature offers the designing of specific drug-target interactions. Despite the discovery of numerous carbamate derivatives that act on the endocannabinoid system (ECS), the development of clinically effective carbamates remains a challenge. In this review, we highlight the therapeutic potential of carbamate inhibitors of endocannabinoid degrading enzymes as a breakthrough in discovering neurotherapeutic drugs. We discuss the design strategies and medicinal chemistry aspects involved in developing carbamate-based molecular architectures that modulate the endocannabinoid signaling pathway by interfering with fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and α/β-Hydrolase domain-containing 6 (ABHD6). Additionally, we highlight the dual activity profile of carbamates against FAAH and MAGL, FAAH and cholinesterase, and FAAH and TRPV1 channels. Furthermore, we illustrate the pharmacophores of O-functionalized carbamates and N-cyclic carbamates that are crucial for FAAH and MAGL inhibitory activities, respectively.

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来源期刊
CiteScore
7.80
自引率
0.00%
发文量
231
审稿时长
6 months
期刊介绍: The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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