Synthesis and evaluation of 2′-substituted cyclobutyl nucleosides and nucleotides as potential anti-HIV agents

Y Li, S Mao, MW Hager, KD Becnel, RF Schinazi…

Index: Li, Yongfeng; Mao, Shuli; Hager, Michael W.; Becnel, Kimberlynne D.; Schinazi, Raymond F.; Liotta, Dennis C. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3398 - 3401

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Citation Number: 18

Abstract

A series of 2′-substituted cyclobutyl nucleoside analogs were efficiently prepared by constructing the core cyclobutyl ring using different [2+ 2] cycloaddition approaches. The triphosphate derivative of a cyclobutyl nucleoside was also synthesized and evaluated against wild-type and mutant HIV reverse transcriptases (RT). Whereas the nucleoside analogs were inactive against HIV-1 in culture, the nucleotide showed good activity not ...