喹诺酮化合物的抗乙型肝炎病毒和丙型肝炎病毒活性

全球有超3亿人携带肝炎病毒,病毒性肝炎是全球第七大死亡原因,每年超100万人因此丧命。未来20年内与病毒性肝炎相关的死亡将继续增加,病毒性肝炎业已成为严重的社会和公共卫生问题。近年来,随着抗病毒药物的广泛使用,乙型肝炎病毒(HBV)和丙型肝炎病毒(HCV)对药物的敏感性不断下降。为克服耐药性,同时降低毒性、提高疗效,亟需研发新型抗乙肝和丙肝药物。喹诺酮类化合物具有潜在的抗HBV和HCV活性,其中的某些化合物如7d和11d具有优秀的活性,极具进一步开发前景。本文将着重介绍近年来喹诺酮类化合物在抗HBV和HCV领域的最新研究进展,并归纳此类药物的构-效关系,以启迪科学家设计活性更高的候选物。

Quinolone Derivatives and Their Activities against Hepatitis B Virus and Hepatitis C Virus

More than 300 million people carry hepatitis viruses. Viral hepatitis which leads to above 1 million deaths annually is the seventh leading cause of death throughout the world. Among them, viral hepatitis type B (caused by hepatitis B virus/HBV) and viral hepatitis type C (caused by hepatitis C virus/HCV) are the most lethal forms. However, the emergency and widely spread of drug-resistant HBV and HCV make the drug less and less effective. Thus, it is imperative to develop new anti-HBV and anti-HCV drugs. Quinolone derivatives possess a variety of biological properties, and some of the exhibited excellent anti-HBV and anti-HCV activities. In particular, compounds 7dand 11ddisplayed promising in vitro activity and favorable pharmacokineticproperties, which could act as ideal starting points for further investigations.This review outlines the recent advances of quinolone derivatives as potential nti-HBV and anti-HCV agents, and summarizes the structure-activity relationship of thesederivatives to provide an insight for rational designs of more active candidates.