摘要
疟疾仍是目前严重威胁人类健康的全球性公共卫生问题,每年近百万人因此丧命。不幸的是,随着耐药性的出现,一线抗疟疾药物的临床疗效逐年下降。因此,对新型抗疟药的研发刻不容缓。香豆素类化合物具有广泛的生物活性,且某些香豆素类化合物已在临床上用于治疗各种疾病。近年来的研究表明,香豆素类化合物具有潜在的体外抗恶性疟原虫和体内抗疟疾活性,引起了药物化学家的广泛关注。本文将归纳近年来香豆素类化合物在抗疟疾领域的研究进展,并讨论这类化合物的构-效关系,为更合理的设计这类抗疟新药提供理论支持。
Malaria remains devastating impact on the health of human populations throughout the world, lead to around 1 million deaths annually. With the emergence and spread of growing resistance, the first-line antimalarials currently used in clinical are more and more ineffective. Therefore, there is an urgent need to develop novel and effective antimalarials. Cormarins, which displayed diverse biological activities, also showed potential in vitro antiplasmodial and in vivo antimalarial profiles. Moreover, some of them are currently used in clinical for treatment of many diseases, making them promising candidates for treatment of malaria. This review aims to outline the recent advances made towards the development of cormarin-containing derivatives as antiplasmodial and antimalarial agents and their structure-activity relationship is also discussed.
出处
《国外医药(抗生素分册)》
CAS
2017年第5期J0058-J0062,共5页
World Notes on Antibiotics
关键词
疟疾
疟原虫
香豆素
杂合体
构-效关系
malaria
plasmodium
coumarin
hybrid
structure-activity relationship