Wilkerson W W, Akamike E, Cheatham W W, Hollis A Y, Collins R D, DeLucca I, Lam P Y, Ru Y
DuPont Merck Pharmaceutical Company, E500/3203 Experimental Station, Wilmington, Delaware 19880-0500, USA.
J Med Chem. 1996 Oct 11;39(21):4299-312. doi: 10.1021/jm9602773.
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 Ki < 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.
已经合成了一系列N，N'-二取代的环状脲3-苯甲酰胺，并对其进行了HIV蛋白酶抑制和抗病毒活性评估。其中一些苯甲酰胺已被证明是HIV蛋白酶的有效抑制剂，其对病毒复制的Ki<0.050 nM，IC90<20 nM，因此可能对艾滋病治疗有用。将讨论该苯甲酰胺系列的合成及其定量构效关系。
