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ID: ALA1146635
Journal: Bioorg Med Chem Lett
Title: Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.
Authors: Kevin NJ, Duffy JL, Kirk BA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.
Abstract: HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P(3) position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment.
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