化学与生物工程
化學與生物工程
화학여생물공정
CHEMISTRY & BIOENGINEERING
2014年
11期
5-11
,共7页
蔡文玺%刘文波%苏发生%王润玲%董卫莉
蔡文璽%劉文波%囌髮生%王潤玲%董衛莉
채문새%류문파%소발생%왕윤령%동위리
乙型肝炎病毒(HBV)%非核苷类%小分子抑制剂
乙型肝炎病毒(HBV)%非覈苷類%小分子抑製劑
을형간염병독(HBV)%비핵감류%소분자억제제
hepatitis B virus(HBV)%non-nucleoside%small molecule inhibitor
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。
慢性乙型肝炎病毒(HBV)感染是許多肝疾病,如肝炎、肝硬化和肝癌的病因,至今仍是影響人類健康的全毬性問題。噹前臨床用藥主要包括免疫調節劑和能抑製逆轉錄酶活性的覈苷類似物,但免疫調節劑的副作用和覈苷類似物的耐受性使得慢性乙型肝炎的臨床治療仍然麵臨著巨大的挑戰,而非覈苷類抗 HBV 藥物的研究為這一現狀的改變提供瞭很大機會。綜述瞭近年來報道的非覈苷類抗 HBV 小分子抑製劑,重點對其化學結構、抗 HBV 活性和構效關繫進行瞭總結。
만성을형간염병독(HBV)감염시허다간질병,여간염、간경화화간암적병인,지금잉시영향인류건강적전구성문제。당전림상용약주요포괄면역조절제화능억제역전록매활성적핵감유사물,단면역조절제적부작용화핵감유사물적내수성사득만성을형간염적림상치료잉연면림착거대적도전,이비핵감류항 HBV 약물적연구위저일현상적개변제공료흔대궤회。종술료근년래보도적비핵감류항 HBV 소분자억제제,중점대기화학결구、항 HBV 활성화구효관계진행료총결。
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 ac-tivity.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 anti-HBV small molecule inhibitors reported recently,focusing on their chemical structures,anti-HBV activities and structure-activity relationships.