Title of article
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1′ substituent
Author/Authors
Joseph L. Duffy، نويسنده , , Brian A. Kirk، نويسنده , , Nancy J. Kevin، نويسنده , , Kevin T. Chapman، نويسنده , , William A. Schleif، نويسنده , , David B. Olsen، نويسنده , , Mark Stahlhut، نويسنده , , Carrie A. Rutkowski، نويسنده , , Lawrence C. Kuo، نويسنده , , Lixia Jin، نويسنده , , Jiunn H. Lin، نويسنده , , Emilio A. Emini، نويسنده , , James R. Tata، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
3323
To page
3326
Abstract
Transposition of the pyridyl nitrogen from the P3 substituent to the P1′ 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 (CIC95) 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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793562
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