Zhou Xiao-Xiong, Littler Eddy
Department of Medicinal Chemistry, Medivir AB, Huddinge, Sweden.
Curr Top Med Chem. 2006;6(9):851-65. doi: 10.2174/156802606777303667.
Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However, the challenges from the resistance and the off-therapy viral rebound are still unmet, and there is a need of developing new therapeutic agents. This review will discuss the structure-activity relationship of the most significant anti-HBV nucleoside analogs and the latest development in the field.
慢性乙型肝炎病毒(HBV)感染影响着全球约4亿人。抑制HBV聚合酶的核苷类似物的开发为治疗HBV感染提供了重要方法。拉米夫定、阿德福韦和恩替卡韦的获批是乙肝治疗的基石。然而,耐药性和停药后病毒反弹带来的挑战仍未得到解决,因此需要开发新的治疗药物。本综述将讨论最重要的抗HBV核苷类似物的构效关系以及该领域的最新进展。