| Literature DB >> 12467630 |
Christopher L Lynch1, Christopher A Willoughby, Jeffrey J Hale, Edward J Holson, Richard J Budhu, Amy L Gentry, Keith G Rosauer, Charles G Caldwell, Ping Chen, Sander G Mills, Malcolm MacCoss, Scott Berk, Liya Chen, Kevin T Chapman, 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, Janet Lineberger, Michael Miller, Emilio A Emini.
Abstract
The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics.Entities:
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Year: 2003 PMID: 12467630 DOI: 10.1016/s0960-894x(02)00829-6
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823