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J Med Chem ; 48(25): 8098-102, 2005 Dec 15.
Article in English | MEDLINE | ID: mdl-16335934

ABSTRACT

Novel HIV-1 protease inhibitors encompassing a tertiary alcohol as part of the transition-state mimicking unit have been synthesized. Variation of the P1'-P3' residues and alteration of the tertiary alcohol absolute stereochemistry afforded 10 inhibitors. High potencies for the compounds with (S)-configuration at the carbon carrying the tertiary hydroxyl group were achieved with Ki values down to 2.4 nM. X-ray crystallographic data for a representative compound in complex with HIV-1 protease are presented.


Subject(s)
Alcohols/chemistry , HIV Protease Inhibitors/chemical synthesis , HIV Protease/chemistry , HIV Protease/metabolism , Cell Line , Cell Membrane Permeability , Crystallography, X-Ray , Drug Resistance, Viral , HIV Protease/genetics , HIV Protease Inhibitors/chemistry , HIV Protease Inhibitors/pharmacology , HIV-1/drug effects , HIV-1/isolation & purification , Humans , Molecular Conformation , Molecular Mimicry , Mutation , Stereoisomerism
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