非核苷类抗乙肝病毒小分子抑制剂的研究进展

Research Progress of Non-Nucleoside Anti-HBV Small Molecule Inhibitors

慢性乙型肝炎病毒(HBV)感染是许多肝疾病,如肝炎、肝硬化和肝癌的病因,至今仍是影响人类健康的全球性问题。当前临床用药主要包括免疫调节剂和能抑制逆转录酶活性的核苷类似物,但免疫调节剂的副作用和核苷类似物的耐受性使得慢性乙型肝炎的临床治疗仍然面临着巨大的挑战,而非核苷类抗HBV药物的研究为这一现状的改变提供了很大机会。综述了近年来报道的非核苷类抗HBV小分子抑制剂,重点对其化学结构、抗HBV活性和构效关系进行了总结。

Hepatitis B virus（HBV）infection is a prime cause of liver diseases such as hepatitis,cirrhosis and hepatocellular carcinoma,and remains a major public health problem in the world.The current drugs clinically available include immunomodulatory agents and nucleoside analogues that inhibit viral reverse transcriptase activity.However,clinical treatment of chronic hepatitis B still face enormous challenges,because of side effects of immunomodulatory agents and viral resistance of nucleoside analogues.Research on non-nucleoside anti-HBV drugs provides a great opportunity to change this condition.This review summarizes some non-nucleoside antiHBV small molecule inhibitors reported recently,focusing on their chemical structures,anti-HBV activities and structure-activity relationships.