Title of article
Cycloalkylpiperazines as HIV-1 protease inhibitors: enhanced oral absorption
Author/Authors
B. Moon Kim، نويسنده , , Ben E. Evans، نويسنده , , Kevin F. Gilbert، نويسنده , , Colleen M. Hanifin، نويسنده , , Joseph P. Vacca، نويسنده , , Stuart R. Michelson، نويسنده , , Paul L. Darke، نويسنده , , Joan A. Zugay، نويسنده , , Emilio A. Emini، نويسنده , , William Schleif، نويسنده , , Jiunn H. Lin، نويسنده , , I. -H. Chen، نويسنده , , Kari Vastag، نويسنده , , Paul S. Anderson، نويسنده , , Joel R. Huff، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1995
Pages
6
From page
2707
To page
2712
Abstract
A series of HIV-1 protease inhibitors containing various acyclic or cyclic alkylpiperazine derivatives were prepared. They exhibit excellent potency in the enzyme inhibition assay and in a whole cell assay demonstrating the lowest CIC95/IC50 ratios observed in the hydroxyethylpiperazine class of inhibitors. Oral pharmacokinetic studies in dogs have been carried out on two compounds in this series and an excellent oral absorption profile was obtained for inhibitor 13, which possesses a cyclopropylpiperazine unit.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1995
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
787771
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