SYNTHESIS AND BIOLOGICAL EVALUATION/ANTIHIV NUCLEOSIDES

描述：(改编自申请者摘要)：尽管 在艾滋病毒感染的治疗方面取得了一些进展， 艾滋病化疗中尚未解决的问题，包括病毒耐药性， 病毒库、抢救疗法和潜在的病毒消除。 为了解决所有这些问题，未来的迫切需要 将发现更有效和更有选择性的新抗艾滋病毒方案 与批准的药物具有不同的耐药性模式。这项建议 是正在进行的药物发现工作在以下领域的继续 佐治亚大学和埃默里大学的抗病毒核苷 大学/退伍军人医学中心。调查人员提议探索 以下几类主要为L核苷的化学和病毒学研究： (2)含氟L-D4N；(3)2-取代 L-碳环核苷(4)L-非离子核苷(5)L-氧杂核苷 类似物；(6)环丁烷碳环L-核苷；(7)构象 限制的环丙基环丙基核苷； 环丙基碳环核苷。

DESCRIPTION: (Adapted from Applicant's Abstract): Despite significant advances in the treatment of HIV infection, there are a number of unresolved issues in AIDS chemotherapy, including viral resistance, viral reservoir, salvage therapy and potential elimination of the virus. In order to solve all these problems, the critical need in the future will be the discovery of more potent and selective new anti-HIV regimens with different patterns of resistance than approved drugs. This proposal is a continuation of ongoing drug discovery efforts in the area of antiviral nucleosides at the University of Georgia and the Emory University/VA Medical Center. The investigators propose to explore the chemistry and virology of the following classes of mainly L-nucleosides: (1) oxaselenolane nucleosides; (2) fluorinated L-D4N; (3) 2-substituted L-carbocyclic nucleosides; (4) L-apionucleosides; (5) L-oxetanocin analogs; (6) cyclobutane carbocyclic L-nucleosides; (7) conformationally restricted endo-cyclopropropylnucleosides; (8) homo- cyclopropylcarbocyclic nucleosides.