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邻苯二甲酰亚胺作为抗炎剂。

Phthalimides as anti-inflammatory agents.

作者信息

Heras Martinez Hector Mario, Barragan Enrique, Marichev Kostiantyn O, Chávez-Flores David, Bugarin Alejandro

机构信息

Department of Chemistry & Physics, Florida Gulf Coast University, Fort Myers, FL, USA.

Facultad de Ciencias Químicas, Universidad Autónoma de Chihuahua, Circuito Universitario, Chihuahua, Mexico.

出版信息

Future Med Chem. 2025 Jan;17(1):125-142. doi: 10.1080/17568919.2024.2437979. Epub 2024 Dec 17.

Abstract

Isoindoline-1,3-dione, also referred as phthalimide, has gained recognition as promising pharmacophore due to the documented biological activities of its derivatives. Phthalimides are a family of synthetic molecules that exhibit notable bioactivity across various fields, particularly as anticancer and anti-inflammatory agents. This review focuses on syntheses and anti-inflammatory studies of the reported phthalimide derivatives. Although there are several synthetic protocols to produce phthalimide derivatives, two methods for synthesizing phthalimides are traditionally used: reacting phthalic anhydride with amines or anilines and the Gabriel synthesis. Due to their structural versatility and established pharmacological effects, derivatives of phthalimides such as the commercially available drugs thalidomide, pomalidomide, and lenalidomide, have driven the development of new derivatives offering hundreds of promising drug candidates with exceptional therapeutic potential, such as LASSBio 468 and adducts , , , , , and to name some.

摘要

异吲哚啉 -1,3 - 二酮,也被称为邻苯二甲酰亚胺,由于其衍生物已被记录的生物活性,作为一种有前景的药效基团而受到认可。邻苯二甲酰亚胺是一类合成分子,在各个领域都表现出显著的生物活性,特别是作为抗癌和抗炎剂。本综述重点关注已报道的邻苯二甲酰亚胺衍生物的合成及抗炎研究。虽然有几种合成邻苯二甲酰亚胺衍生物的方案,但传统上使用两种合成邻苯二甲酰亚胺的方法:使邻苯二甲酸酐与胺或苯胺反应以及盖布瑞尔合成法。由于其结构的多样性和已确定的药理作用,邻苯二甲酰亚胺的衍生物,如市售药物沙利度胺、泊马度胺和来那度胺,推动了新衍生物的开发,提供了数百种具有卓越治疗潜力的有前景的候选药物,如LASSBio 468以及加合物 、 、 、 、 等,仅举几例。

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