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咖啡酸衍生物、类似物及其应用:专利研究综述(2009-2013)。

Caffeic acid derivatives, analogs and applications: a patent review (2009-2013).

机构信息

University of Porto, CIQ/Department of Chemistry and Biochemistry, Faculty of Sciences , Rua do Campo Alegre s/n, Porto , Portugal

出版信息

Expert Opin Ther Pat. 2014 Nov;24(11):1257-70. doi: 10.1517/13543776.2014.959492. Epub 2014 Oct 4.

Abstract

INTRODUCTION

Caffeic acid (CA) is broadly distributed in several species of the plant kingdom and is widely consumed in human diet. CA and derivatives have been extensively studied in the past years, which unveiled a broad spectrum of biological activities and potential therapeutic applications. As a result, there has been an upsurge in the development of new chemical entities based on the CA scaffold.

AREAS COVERED

The scope of this review is to revisit the therapeutic potential of CA and derivatives. It provides an overview of patented processes and applications thereof between 2009 and 2013.

EXPERT OPINION

The phenylpropanoid framework is currently considered a valid structure for drug discovery programs. Actually, CA has been widely used as a template for the development of new chemical entities with potential therapeutic interest in human diseases associated with oxidative stress. Additionally, the applicability of CA derivatives expands to the realms of cosmetic industry due to its stabilizing properties. The synthesis of esters, amides and hybrids with currently marketed drugs is a trending strategy for the development of derivatives with therapeutic application. It is our opinion that the innovative artwork currently being developed involving this chemical scaffold will yield new and effective therapeutic agents in a foreseeable future.

摘要

简介

咖啡酸(CA)广泛分布于植物界的多个物种中,并且在人类饮食中广泛摄入。过去几年中,CA 及其衍生物已得到广泛研究,揭示了其广泛的生物活性和潜在的治疗应用。因此,基于 CA 支架的新化学实体的开发呈现出激增的趋势。

涵盖范围

本综述的范围是重新审视 CA 和衍生物的治疗潜力。它概述了 2009 年至 2013 年期间已获得专利的工艺及其应用。

专家意见

苯丙烷骨架目前被认为是药物发现计划的有效结构。实际上,CA 已被广泛用作开发具有治疗潜力的新化学实体的模板,这些实体对与氧化应激相关的人类疾病具有潜在的治疗作用。此外,由于其稳定性能,CA 衍生物的适用性扩展到化妆品行业领域。与目前市售药物的酯、酰胺和杂种的合成是开发具有治疗应用的衍生物的趋势策略。我们认为,在可预见的未来,涉及这种化学支架的创新艺术作品将产生新的、有效的治疗剂。

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