Title of article
Thiophene derivatives as extremely high affinity P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors
Author/Authors
B. Moon Kim، نويسنده , , James P. Guare، نويسنده , , Joseph D. 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. W. 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
185
To page
190
Abstract
A series of hydroxyethylpiperazine HIV-1 protease inhibitors containing various monocyclic or bicyclic thienylmethyl substituents as P3′ ligands were prepared. They were found to exhibit extremely high potency in the enzyme inhibition assay. These inhibitors also proved to be highly effective against viral spread in a whole cell assay. Some representative compounds in this series have been examined for oral bioavailability in dogs and the pharmacokinetic properties were found to be somewhat related to their aqueous solubilities.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1995
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
787305
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