Title of article
Substituted alkylpyridines as P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles
Author/Authors
B. Moon Kim، نويسنده , , Colleen M. Hanifin، نويسنده , , C. Blair Zartman، نويسنده , , Joseph P. Vacca، نويسنده , , Stuart R. Michelson، نويسنده , , Jiunn H. Lin، نويسنده , , I. -H. Chen، نويسنده , , Kari Vastag، نويسنده , , Paul L. Darke، نويسنده , , Joan A. Zugay، نويسنده , , Emilio A. Emini، نويسنده , , William Schleif، نويسنده , , Paul S. Anderson، نويسنده , , Joel R. Huff، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1995
Pages
6
From page
2239
To page
2244
Abstract
As a systematic approach to develop HIV-1 protease inhibitors exhibiting desirable pharmacokinetic profiles, hydroxyethylpiperazine series of inhibitors containing various mono- or dialkyl-substituted pyridylmethyl groups have been examined. Very high enzyme inhibitory potency and antiviral activity in a whole cell assay were observed with these inhibitors and, when administered orally to dogs, selected compounds in this series exhibited prolonged half-lives compared to the non-substituted pyridylmethyl compound 1.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1995
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
787688
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