Title of article
Isophthalic acid derivatives: amino acid surrogates for the inhibition of HIV-1 protease
Author/Authors
Stephen W. Kaldor، نويسنده , , Bruce A. Dressman، نويسنده , , Marlys Hammond، نويسنده , , J Ernest Villafranca and Krzysztof Appelt، نويسنده , , Jeffrey A. Burgess، نويسنده , , Penny P. Lubbehusen، نويسنده , , Mark A. Muesing، نويسنده , , Steven D. Hatch، نويسنده , , Mary Ann Wiskerchen، نويسنده , , Angela J. Baxter، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1995
Pages
6
From page
721
To page
726
Abstract
Using the X-ray crystal structure of the inhibitor 1 complexed to HIV-1 protease, a new series of HIV-1 protease inhibitors was developed incorporating substituted isophthalic acid derivatives as amino acid surrogates. Through iterative structure-based design, the lead compound 2 was optimized to produce a variety of non-peptide HIV-1 protease inhibitors with significant antiviral activity. In contrast to 1, several members of this series exhibit significant oral absorption in animals.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1995
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
787404
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