Laboratorio de Diversidade Molecular e Quimica Medicinal (LaDMol-QM, Molecular Diversity and Medicinal Chemistry Laboratory), Departament of Chemistry, Universidade Federal Rural do Rio de Janeiro, Seropedica, Rio de Janeiro, 239897-000, Brazil.
Curr Top Med Chem. 2018;18(2):124-148. doi: 10.2174/1568026618666180329115523.
Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and receptors in live organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarins compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, anti-diabetics, anti-inflammatory, antibacterial, antifungal and anti-neurodegerative agents. Additionally, it also includes applications of coumarins as fluorescent sensors for biological systems. Thus, this work aims to contribute to the development of new rational research projects for the treatment and diagnosis of pathologies using coumarin derivatives.
香豆素是一类广泛分布于植物、部分真菌和细菌中的天然产物,化学结构为 1,2-苯并吡喃酮。目前,许多合成方法可以发现具有扩展化学空间的香豆素。香豆素能够与生物体中的许多酶和受体发生非共价相互作用,从而表现出广泛的生物活性和应用。本文概述了香豆素类化合物在治疗多种疾病的药物化学中的应用。选择了近年来关于香豆素作为抗凝剂、抗癌、抗氧化、抗病毒、抗糖尿病、抗炎、抗菌、抗真菌和抗神经退行性疾病药物的重要活性的相关重要实例。此外,还包括香豆素作为生物体系荧光传感器的应用。因此,本工作旨在为使用香豆素衍生物治疗和诊断疾病的新的合理研究项目的开发做出贡献。