靶向分枝菌酸生物合成的抗结核化合物研究进展  

Recent Advances in Antitubercular Compounds Targeting Mycolic Acid Biosynthesis and Transport

作　　者：吕润秋 张维 于丽芳 LV Runqiu;Zhang Wei;Yu Lifang(Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development,School of Chemistry and Molecular Engineering,East China Normal University,Shanghai 200062)

机构地区：[1]华东师范大学化学与分子工程学院上海分子治疗与新药创制工程技术研究中心,上海200062

出　　处：《有机化学》2021年第6期2249-2260,共12页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21778019)资助项目。

摘　　要：结核病近年来已超过艾滋病成为当今世界范围内致死率高的感染性疾病之一.结核病耐药问题严峻,耐多药结核病治愈率低、治疗方案复杂且周期长.抗耐药结核领域存在重大研究机遇,亟需发现与发展针对新靶点的新化学实体.分枝菌酸的生物合成和转运途径富含抗结核药物的有效靶点,综述了靶向该途径的抑制剂,讨论了其作用机制、药代动力学性质等最新研究进展.Tuberculosis is now recognized as the most fatal infectious disease worldwide,eclipsing HIV in recent years.Drug-resistance tuberculosis continues to be a severe public crisis.The cure rate in persons with multidrug-resistant tuberculosis(MDR-TB)is unacceptably low,and the treatment of MDR-TB requires complex treatment regimens over a long period.There is a great opportunity in the field of tuberculosis as novel chemical entities with different mechanisms of action are particularly needed.The biosynthesis and transport pathways of mycolic acid represents a well proven and effective target for chemical intervention for TB.This article reviews the important inhibitors targeting to this pathway,as well as the recent research advances in the mechanism and pharmacokinetic properties etc.

关 键 词：耐药结核病 分枝菌酸的生物合成及转运途径 重要靶点 抑制剂 

分 类 号：TQ460.1[化学工程—制药化工]