香豆素杂合体的抗结核活性研究进展  

The Research Progress of Coumarin Hybrids with Anti-tubercular Potential

作　　者：蒋丹 张强 Jiang Dan;Zhang Qiang(School of Nuclear Technology and Chemical&Biology,Hubei University of Science and Technology,Xianning 437000;Hubei Jingmen Rehabilitation Hospital,Jingmen 448000)

机构地区：[1]湖北科技学院核技术与化学生物学院,咸宁437000 [2]湖北荆门康复医院,荆门448000

出　　处：《国外医药（抗生素分册）》2023年第5期346-353,共8页World Notes on Antibiotics

摘　　要：结核病是由结核分枝杆菌复合群引起的重大传染性疾病,严重威胁人类的生命健康。其中,结核分枝杆菌是最主要的致病菌,且以感染肺部为主,故结核病又称肺结核。一线抗结核药物已在临床上使用超过半个世纪,尽管目前仍不可或缺,但随着新型耐药结核如耐多药结核、广泛耐药结核和完全耐药结核的不断涌现,使得一线抗结核药物的疗效逐年下降。因此,研发新的抗结核药物一直是新药研发领域的重点之一。药物化学家进行了不懈的努力,但自利福平问世以来,进入临床试验的化合物屈指可数,被批准上市的新药更是少之又少。香豆素类化合物具有包括抗结核在内的多种生物活性,其中的某些化合物对耐药结核分枝杆菌也显示出良好的活性,极具进一步研究价值。本文将重点介绍2018年1月—2023年1月首次报道的具有抗结核活性的香豆素杂合体的最新研究进展,并归纳其构—效关系,以启迪药物化学家设计合成活性更高、毒副作用更低的抗结核候选物。Tuberculosis,an infectious disease caused by the Mycobacterium tuberculosis complex,seriously threatens human health.Among them,Mycobacterium tuberculosis is the major pathogen and mainly infects pulmonary.Thus,tuberculosis is also called pulmonary tuberculosis.First-line anti-tubercular drugs have been used clinically for more than 50 years and are still indispensable at present,but the efficacy of first-line anti-tubercular drugs has declined year by year with the continuous emergence of new drug-resistant tuberculosis such as multidrugresistant,extensively drug-resistant and totally drug-resistant tuberculosis.Therefore,one of the first priority for new drug research and development has always been the creation of new anti-tubercular medications.However,few candidates have entered clinical trials and been approved for marketing since the introduction of rifampicin.Coumarins have a variety of biological activities,including anti-tuberculosis and some of them also possess excellent activity against drug-resistant Mycobacterium tuberculosis.Hence,coumarins are useful scaffolds for the discovery of novel anti-tubercular drugs.In order to motivate medicinal chemists to create and synthesize new candidates with higher activity and lower toxicity and side effects,this paper will concentrate on the most recent research developments of coumarin hybrids with anti-tubercular activity developed since 2018 and summarize their structureactivity relationships.

关 键 词：香豆素 杂合体 结核 耐药结核 构—效关系 

分 类 号：R978.3[医药卫生—药品]