L-核苷类抗HIV、HBV活性化合物研究进展

抗病毒新试剂的不断涌现,为HIV、HBV感染者的临床治疗提供了有效的方法.在抗病毒试剂中,核苷类化合物占据了十分重要的地位.本文阐述了核苷类化合物抗病毒的作用机理,介绍了L型核苷的发展历史及一些新型具有抗HIV、HBV生物活性的L型核苷类化合物的分类.同时,通过对一些新型具有抗HIV、HBV生物活性的核苷类化合物如BCH、FTC、OddC、d4A、Fd4C等,D型和L型不同对映异构体抗病毒活性及生物毒性的对比发现,L型异构体比其相应的D型异构体具有抗病毒活性更高、生物毒性更低的特点.药物化学家们对此产生了极大的兴趣,进一步开展了新型L型核苷类化合物设计、合成的相关研究,以便筛选出更安全有效的抗病毒试剂.

Advances in L-Nucleosides as Anti-HIV and Anti-HBV Agents

Drug discovery for anti-HIV, anti-HBV chemotherapy has provided the effective clinical treatment. Among these antiviral agents used in therapy, nucleoside analogues are particularly useful. In this paper, the antiviral mechanism of the nucleoside analogues, the discovery of L-nucleoside and the classification of some new anti-HIV, anti-HBV L-nucleoside analogues are introduced. In addition, the datum of two enantiomers of some anti-HIV, anti-HBV nucleoside analogues indicate that the bioactivities and securities of L-nucleoside analogues is superior to the counterpart enantiomers. As a result, the medicinal chemists have focused their attention on designing and preparing new L-nucleoside analogues to search for more powerful and securer new antiviral agents.