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生物活性肉桂酸衍生物合成方法的最新进展。

Recent advances in synthetic approaches for bioactive cinnamic acid derivatives.

作者信息

Kustiana Betty A, Widiyarti Galuh, Ernawati Teni

机构信息

Research Center for Pharmaceutical Ingredients and Traditional Medicine, National Research and Innovation Agency of Indonesia (BRIN), KST BJ Habibie, Kawasan Puspiptek, 452 Building, Tangerang Selatan 15314, Indonesia.

出版信息

Beilstein J Org Chem. 2025 May 28;21:1031-1086. doi: 10.3762/bjoc.21.85. eCollection 2025.

Abstract

Cinnamic acid derivatives represent a significant class of biologically active compounds exhibiting a broad spectrum of activities, such as antifungal, antidengue, antimetastatic, antimicrobial, antibacterial, and anticancer properties. Their preparation has attracted considerable attention due to their versatile applications across the pharmaceutical, food, and chemical sectors. This review elucidates the functional groups of cinnamic acid that are instrumental in the rational design of biologically active derivatives. A comprehensive representative of recent advancements in synthetic methodologies over the past five years is presented, particularly emphasizing the active scaffolds of bioactive cinnamic acid derivatives. The review provides a strategic overview of alternative synthetic routes and highlights the latest innovations, including more efficient, highly selective, and environmentally sustainable approaches. Given the widespread incorporation of the cinnamic acid framework in various therapeutic agents, this review delivers critical insights into a molecular design for hit-to-lead optimization, offering detailed synthetic strategies for diverse functional modifications. By critically examining these methodologies, the paper underscores their role in expanding the utility of cinnamic acid derivatives and addressing prevailing challenges.

摘要

肉桂酸衍生物是一类重要的生物活性化合物,具有广泛的活性,如抗真菌、抗登革热、抗转移、抗菌、抗细菌和抗癌特性。由于其在制药、食品和化工领域的广泛应用,它们的制备引起了相当大的关注。本综述阐明了肉桂酸的官能团,这些官能团有助于合理设计生物活性衍生物。本文介绍了过去五年合成方法的全面代表性进展,特别强调了生物活性肉桂酸衍生物的活性支架。该综述提供了替代合成路线的战略概述,并突出了最新的创新,包括更高效、高选择性和环境可持续的方法。鉴于肉桂酸框架在各种治疗剂中的广泛应用,本综述为从先导化合物到候选药物的优化提供了关键的分子设计见解,为各种功能修饰提供了详细的合成策略。通过批判性地审视这些方法,本文强调了它们在扩大肉桂酸衍生物的用途和应对现有挑战方面的作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd3e/12130629/792b86a14eb9/Beilstein_J_Org_Chem-21-1031-g002.jpg

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