Suppr超能文献

N-取代-2,4-噻唑烷二酮在各种病理状况中的应用。

Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions.

机构信息

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi-Mumbai, India.

出版信息

Mini Rev Med Chem. 2019;19(4):346-360. doi: 10.2174/1389557518666171129163426.

Abstract

Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and -NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.

摘要

噻唑烷-2,4-二酮(TZD)是最常见的杂环之一,它被用于设计和合成各种致病条件的实体,包括癌症。自发现以来,已经对 5 位进行了各种取代,并进行了综述。5 位的各种取代导致了噻唑烷二酮类化合物的产生,其靶点过氧化物酶体增殖物激活受体 γ(PPARγ)在发现它们十年后才被发现。TZD 的酸性氢(-NH)是激活 PPARγ 的主要药效团要求。然而,先进的计算技术已经帮助设计了在 TZD 的亚甲基和-NH 基团上带有取代基的化合物,这些化合物针对涉及各种病理情况的酶,例如糖尿病、高血脂、传染病、炎症和癌症。在上述治疗领域中,亚甲基和 N-取代的 TZD 表现出的有希望的活性促使我们收集信息,这将帮助研究人员改变现有配体的结构,并设计具有更好的安全性和疗效特征的新 TZD 衍生物。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验