Title of article
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains
Author/Authors
Dong-Ming Shen، نويسنده , , Min Shu، نويسنده , , Sander G. Mills، نويسنده , , Kevin T. Chapman، نويسنده , , Lorraine Malkowitz، نويسنده , , Martin S. Springer، نويسنده , , Sandra L. Gould، نويسنده , , Julie A. DeMartino، نويسنده , , Salvatore J. Siciliano، نويسنده , , Gloria Y. Kwei، نويسنده , , Anthony Carella، نويسنده , , Gwen Carver، نويسنده , , Karen Holmes، نويسنده , , William A. Schleif، نويسنده , , Renee Danzeisen، نويسنده , , Daria Hazuda، نويسنده , , Joseph Kessler، نويسنده , , Janet Lineberger، نويسنده , , Michael D. Miller، نويسنده , , Emilio A. Emini، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
935
To page
939
Abstract
Replacement of the flexible connecting chains between the piperidine moiety and an aromatic group in previous CCR5 antagonists with heterocycles, such as pyrazole and isoxazole, provided potent CCR5 antagonists with excellent anti-HIV-1 activity in vitro. SAR studies revealed optimal placement of an unsubstituted nitrogen atom in the heterocycle to be meta to the bond connected to the 4-position of piperidine. Truncation of a benzyl group to a phenyl group afforded compounds with dramatically improved oral bioavailability, albeit with reduced activity.
Keywords
fax: +1-732-594- , HIV-1 , antiviral , Pyrazole.* Corresponding author. Tel.: +1-732-594-7303 , CCR5 antagonists
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794105
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