Effects of Aryl Substituents on the Anti-HIV Activity of the Arylphosphoramidate Derivatives of Stavudine
2002 ◽
Vol 13
(3)
◽
pp. 197-203
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Keyword(s):
Anti Hiv
◽
We compared the anti-HIV activity of 13 phenyl phosphate derivatives of stavudine (2′,3′-didehydro-2′,3′-dideoxythymidine/d4T) by examining their ability to inhibit HIV-1 replication in human peripheral blood mononuclear cells. Our results show that the introduction of electron-withdrawing substituents enhances the activity of these phosphoramidate derivatives. The rate of chemical hydrolysis under alkaline conditions (but not the lipophilicity) predicted the potency of the compounds.
1995 ◽
Vol 121
(S1)
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pp. S37-S37