【作者】 展鹏； 李潇； 刘新泳；

【机构】 山东大学药学院药物化学研究所；

【摘要】 艾滋病(AIDS)在全世界传播以来,给人类的健康和生命带来了巨大的威胁。由于目前临床药物严重的耐药性问题及长期应用的毒副作用,研发高效抗耐药的抗艾滋病药物及全新疗法是当前药物化学领域的研究热点。近年来,多靶点和多价态结合药物越来越受到研究者的关注,并且成为合理设计抗艾滋病药物的新途径。本文通过代表性实例综述了合理设计多靶点及多价态抗艾滋病药物的新进展,并对目前存在问题和研究趋势进行了总结和展望,为进一步研究提供了重要信息。更多还原

【Abstract】 Human immunodeficiency virus type 1(HIV-1) is the etiological agent of acquired immunodeficiency syndrome(AIDS).Emergence of drug-resistant HIV-1 mutants and side effects impede the long-term usage of drugs,requiring a significant need for new strategies of drug discovery and alternative therapeutic agents or protocols.More recently,among the most promising strategies,design of multitarget-directed ligands(MTDLs) and multivalent ligands has gained increasing acceptance.The exploration of MTDLs and multivalent ligands strategy should be valuable in anti-HIV drug discovery.In this article,current knowledge,challenges and outlook for the rational design of the multitarget and multivalent anti-HIV agents are described and a number of illustrative examples are given to highlight the representative rational design paradigms,and to help medicinal chemists discover the next generation of anti-HIV agents.更多还原