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ID: ALA1136139
Journal: Bioorg Med Chem Lett
Title: The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.
Authors: Zhang F, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.
Abstract: Replacement of the pyridylmethyl moiety in indinavir with a pyridyl oxazole yielded HIV-1 protease inhibitors (PI) with greatly improved potency against PI-resistant HIV-1 strains. A meta-methoxy group on the pyridyl ring and a gem-dimethyl methyl linkage afforded compound 10 with notable in vitro antiviral activity against HIV-1 viral strains with reduced susceptibility to the clinically available PIs. Compound 10 also demonstrated favorable in vivo pharmacokinetics in animal models.
CiteXplore: 12852969