Synthesis and antiviral activity of methyl derivatives of 9-[2-(phosphonomethoxy) ethyl] guanine

…, V Brankovan, R Datema, MJM Hitchcock…

文献索引：Yu; Bronson; Yang; Patick; Alam; Brankovan; Datema; Hitchcock; Martin Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2958 - 2969

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被引用次数: 48

摘要

A number of methyl derivatives of 9-[2-(phosphonomethoxy) ethyl] guanine (PMEG, 1) have been synthesized and tested in vitro for anti-herpes and anti-human immunodeficiency virus (HIV) activity. Among these analogues,(R)-a'-methyl-PMEG [(R)-31 and Z', B'-dimethyl- PMEG (7) demonstrated potent anti-HIV activity in the XTT assay with ECW values of 1.0 and 2.6 pM, respectively. The corresponding (S)-2'-methyl-PMEG [(S)-31 was found to be leas ...