3'-叠氮基-2',3'-双脱氧嘌呤核苷的合成与评价及其作为人类免疫缺陷病毒抑制剂的研究。
Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus.
机构信息
Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Atlanta, GA 30033, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):60-4. doi: 10.1016/j.bmcl.2009.11.031. Epub 2009 Nov 13.
Abstract
Based on the promising drug resistance profile and potent anti-HIV activity of beta-d-3'-azido-2',3'-dideoxyguanosine, a series of purine modified nucleosides were synthesized by a chemical transglycosylation reaction and evaluated for their antiviral activity, cytotoxicity, and intracellular metabolism. Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes.
摘要
基于 β-D-3'-叠氮-2',3'-二脱氧鸟苷有前途的耐药性特征和强大的抗 HIV 活性，通过化学转糖基反应合成了一系列嘌呤修饰核苷，并评估了它们的抗病毒活性、细胞毒性和细胞内代谢。在所合成的化合物中，有几种在原代淋巴细胞中表现出强大和选择性的抗 HIV 活性。
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