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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. | LitMetric
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

Christopher L Lynch Jeffrey J Hale Richard J Budhu Amy L Gentry Sander G Mills Kevin T Chapman Malcolm MacCoss Lorraine Malkowitz Martin S Springer Sandra L Gould Julie A DeMartino Salvatore J Siciliano Margaret A Cascieri Anthony Carella Gwen Carver Karen Holmes William A Schleif Renee Danzeisen Daria Hazuda Joseph Kessler

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.

Published: October 2002

A series of alpha-(pyrrolidin-1-yl)acetic acids is presented as selective and potent antivirals against HIV. Several of the pyrrolidine zwitterions demonstrated reasonable in vitro properties, enhanced antiviral activities and improved pharmacokinetic profiles over pyrrolidine 1.

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http://dx.doi.org/10.1016/s0960-894x(02)00606-6DOI Listing

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