摘要
β-内酰胺类化合物不仅是临床上使用最为广泛的广谱抗生素,还具有抗结核、抗肿瘤、抗炎、抗氧化、抗病毒和抗疟疾等多种生物活性。其中,β-内酰胺类化合物在抗疟疾领域的应用引起了药物化学家的持续关注。本文将着重介绍近年来β-内酰胺类化合物在抗疟疾领域的研究进展,并讨论此类化合物的构-效关系,为寻找疗效更高、毒副作用更小的β-内酰胺类抗疟疾新药提供理论依据。
β-Lactam derivatives are emerged as one of the widest used antibiotics. Apart from their traditional broad antibacterial activity, β-lactam derivatives exhibited diverse pharmacological properties such as anti-TB, anti-tumor, anti-inflammatory, anti-oxidant, anti-virus, antiplasmodial and antimalarial activities. Hereinto, the antiplasmodial and antimalarial activities of β-lactam derivatives caused continuous interests. This review aims to summarize the recent advances made towards the discovery of antiplasmodial and antimalarial derivatives holding β-lactam motif to provide an insight for rational designs of more active and less toxic antimalarials.
出处
《国外医药(抗生素分册)》
CAS
2017年第5期J0011-J0016,共6页
World Notes on Antibiotics
关键词
疟疾
疟原虫
Β-内酰胺
杂合体
构.效关系
antimalarial: antiplasmodial: β-lactam
hybrids
structure-activity relationship