HIV Protease Inhibitory Bis-benzamide Cyclic Ureas: A Quantitative Structure−Activity Relationship Analysis
摘要:
A series of N,N'-disubstituted cyclic urea 3-benzamides has been synthesized and evaluated for HIV protease inhibition and antiviral activity. Some of these benzamides have been shown to be potent inhibitors of HIV protease with K-i < 0.050 nM and IC90 < 20 nM for viral replication and, as such, may be useful in the treatment of AIDS. The synthesis and quantitative structure-activity relationship for this benzamide series will be discussed.
Nonsymmetrically Substituted Cyclic Urea HIV Protease Inhibitors
作者:Wendell W. Wilkerson、Scott Dax、Walter W. Cheatham
DOI:10.1021/jm970288b
日期:1997.12.1
A series of nonsymmetrically substituted cyclic ureacarboxamides was synthesized and evaluated for antiviral activity as a function of the inhibition of HIV-protease. Selected proteaseinhibitors were also evaluated for oral bioavailability. The synthesis, pharmacology, quantitative structure-activity relationship (QSAR), and pharmacokinetics for the series will be discussed.
HIV Protease Inhibitory Bis-benzamide Cyclic Ureas: A Quantitative Structure−Activity Relationship Analysis
作者:Wendell W. Wilkerson、Emeka Akamike、Walter W. Cheatham、Andrea Y. Hollis、R. Dale Collins、Indawati DeLucca、Patrick Y. S. Lam、Yu Ru
DOI:10.1021/jm9602773
日期:1996.1.1
A series of N,N'-disubstituted cyclic urea 3-benzamides has been synthesized and evaluated for HIV protease inhibition and antiviral activity. Some of these benzamides have been shown to be potent inhibitors of HIV protease with K-i < 0.050 nM and IC90 < 20 nM for viral replication and, as such, may be useful in the treatment of AIDS. The synthesis and quantitative structure-activity relationship for this benzamide series will be discussed.