Nonsymmetrically substituted cyclic urea HIV protease inhibitors.

Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
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DOI:
10.1002/chin.199815166
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发表时间:
1997-12
影响因子:
7.3
通讯作者:
W. W. Wilkerson-W.;S. Dax;W. W. Cheatham-W.
W. W. Wilkerson-W.;S. Dax;W. W. Cheatham-W.
中科院分区:
医学1区
文献类型:
--
作者:
W. W. Wilkerson-W.;S. Dax;W. W. Cheatham-W.

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合成了一系列不对称取代的环状尿素酰胺类化合物,并评价了它们的抗病毒活性与抑制HIV-蛋白酶的关系。还对选定的蛋白水解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、定量构效关系(QSAR)和药代动力学。
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.