非对称取代的环脲类HIV蛋白酶抑制剂。
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
作者信息
Wilkerson W W, Dax S, Cheatham W W
机构信息
DuPont Merck Pharmaceutical Company, Experimental Station, Wilmington, Delaware 19880-0500, USA.
出版信息
J Med Chem. 1997 Dec 5;40(25):4079-88. doi: 10.1021/jm970288b.
PMID:9406598
Abstract
A series of nonsymmetrically substituted cyclic ureacarboxamides was synthesized and evaluated for antiviral activity as a function of the inhibition of HIV-protease. Selected protease inhibitors were also evaluated for oral bioavailability. The synthesis, pharmacology, quantitative structure-activity relationship (QSAR), and pharmacokinetics for the series will be discussed.
摘要
合成了一系列非对称取代的环状脲羧酰胺，并根据其对HIV蛋白酶的抑制作用评估了抗病毒活性。还对选定的蛋白酶抑制剂进行了口服生物利用度评估。将讨论该系列化合物的合成、药理学、定量构效关系（QSAR）和药代动力学。
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