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. 2003 Oct 6;13(19):3323-6.
doi: 10.1016/s0960-894x(03)00680-2.

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent

Joseph L Duffy  1 , Brian A Kirk, Nancy J Kevin, Kevin T Chapman, William A Schleif, David B Olsen, Mark Stahlhut, Carrie A Rutkowski, Lawrence C Kuo, Lixia Jin, Jiunn H Lin, Emilio A Emini, James R Tata
Affiliations

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent

Joseph L Duffy et al. Bioorg Med Chem Lett. .

Abstract

Transposition of the pyridyl nitrogen from the P(3) substituent to the P(1)' substituent in HIV-1 protease inhibitors (PI) affords compounds such as 3 with an improved inhibitory profile against multiple P450 isoforms. These compounds also displayed increased potency, with 3 inhibiting viral spread (CIC(95)) at <8 nM for every strain of PI-resistant HIV-1 tested. The poor to modest bioavailability of these compounds may correlate in part to their aqueous solubility.

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