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邻苯二甲酰亚胺作为一种多功能的药效团骨架:揭示其多样的生物活性。

Phthalimide as a versatile pharmacophore scaffold: Unlocking its diverse biological activities.

机构信息

Department of Chemistry, University College London (UCL), London, UK.

School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, São Paulo, Brazil.

出版信息

Drug Dev Res. 2023 Nov;84(7):1346-1375. doi: 10.1002/ddr.22094. Epub 2023 Jul 26.

Abstract

Phthalimide, a pharmacophore exhibiting diverse biological activities, holds a prominent position in medicinal chemistry. In recent decades, numerous derivatives of phthalimide have been synthesized and extensively studied for their therapeutic potential across a wide range of health conditions. This comprehensive review highlights the latest developments in medicinal chemistry, specifically focusing on phthalimide-based compounds that have emerged within the last decade. These compounds showcase promising biological activities, including anti-inflammatory, anti-Alzheimer, antiepileptic, antischizophrenia, antiplatelet, anticancer, antibacterial, antifungal, antimycobacterial, antiparasitic, anthelmintic, antiviral, and antidiabetic properties. The physicochemical profiles of the phthalimide derivatives were carefully analyzed using the online platform pkCSM, revealing the remarkable versatility of this scaffold. Therefore, this review emphasizes the potential of phthalimide as a valuable scaffold for the development of novel therapeutic agents, providing avenues for the exploration and design of new compounds.

摘要

酞酰亚胺作为一种具有多种生物活性的药效团,在药物化学中占有重要地位。在过去的几十年中,已经合成了许多酞酰亚胺衍生物,并对它们在广泛的健康状况下的治疗潜力进行了广泛的研究。本综述重点介绍了药物化学的最新进展,特别是在过去十年中出现的基于酞酰亚胺的化合物。这些化合物具有有前途的生物活性,包括抗炎、抗老年痴呆症、抗癫痫、抗精神分裂症、抗血小板、抗癌、抗菌、抗真菌、抗结核分枝杆菌、抗寄生虫、驱虫、抗病毒和抗糖尿病特性。使用在线平台 pkCSM 仔细分析了酞酰亚胺衍生物的物理化学特性,揭示了该支架的显著多功能性。因此,本综述强调了酞酰亚胺作为开发新型治疗剂的有价值支架的潜力,为探索和设计新化合物提供了途径。

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