靛红二聚体和杂合体的抗结核活性研究进展  

The Research Progress of Isatin Dimers and Hybrids with Anti-tubercular Potential

作　　者：徐志 周威 赵诗佳 Xu Zhi;Zhou Wei;Zhao Shi-jia(Guizhou University of Traditional Chinese medicine,Guiyang 550025;School of Pharmacy,Guizhou Medical University,Guiyang 550025;School of Chemistry and Chemical Engineering,Wuhan University of Science and Technology,Wuhan 430081)

机构地区：[1]贵州中医药大学,贵阳550025 [2]贵州医科大学药学院,贵阳550025 [3]武汉科技大学化学与化工学院,武汉430081

出　　处：《国外医药（抗生素分册）》2023年第5期327-336,共10页World Notes on Antibiotics

基　　金：贵州省教育厅高校重点领域项目[KY字(2021)048];贵州省卫生健康委科学技术基金(gzwkj2021-451);贵州省科技支撑计划项目[黔科合支撑(2021)一般415];贵州省自然科学基金[黔科合基础(2020)1Y404];贵州省大学生创新创业训练计划项目(S202110662003,S202110662013)。

摘　　要：结核病被认为是由单一传染源引起的最致命的疾病之一,严重威胁人类生命健康,目前已成为全球最受关注的重大公共卫生问题之一。传统的一线抗结核药物具有疗效好和毒副作用低等优点,拯救了无数人的生命。然而,随着单耐药、多耐药、耐多药和广泛耐药结核的不断涌现和广泛传播,一线抗结核药物的疗效不断下降。因此,亟须开发新型抗结核药物。不幸的是,近几十年来鲜有新型抗结核药物上市,反映出该领域的机遇与挑战。靛红类化合物具有包括抗结核在内的多种生物活性且毒副作用小,引起了药物化学家的广泛关注。其中,靛红二聚体和杂合体具有结构多样性和可作用于多个靶点等优点,对药敏型和耐药结核均显示出潜在的活性,是寻找新型抗结核药物的良好结构骨架。本文将综述2017—2022年间所研发的具有潜在抗结核活性的靛红二聚体和杂合体的最新研究进展,为进一步研究提供参考。Tuberculosis is one of the deadliest diseases caused by a single infectious agent,which seriously threatens human life and health and has become one of the most concerned major public health problems in the world.Traditional first-line anti-tubercular drugs demonstrated excellent therapeutic efficacy and low side effects,which have saved countless lives.However,with the continuous emergence and widespread of drug-resistant tuberculosis,the efficacy of first-line anti-tubercular drugs has been declining.Therefore,it's imperative to develop new antitubercular drugs.Unfortunately,there are only a few new anti-tubercular drugs have been launched in recent decades,reflecting the opportunities and challenges in this field.Isatin compounds possess a variety of biological properties,including anti-tubercular activity,and the side effects are low.Consequently,isatin derivatives have attracted extensive attention.Among them,isatin dimers and hybrids have the advantages of structural diversity and can act on multiple drug targets,which show potential activity against both drug-sensitive and drug-resistant tuberculosis.This review provides a reference for future research by summarizing the most recent developments in the development of isatin dimers and hybrids with anti-tubercular potential from 2017 to 2022.

关 键 词：靛红 二聚体 杂合体 结核 构—效关系 

分 类 号：R978.3[医药卫生—药品]