1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains |
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| Authors: | Lynch Christopher L Willoughby Christopher A Hale Jeffrey J Holson Edward J Budhu Richard J Gentry Amy L Rosauer Keith G Caldwell Charles G Chen Ping Mills Sander G MacCoss Malcolm Berk Scott Chen Liya Chapman Kevin T Malkowitz Lorraine Springer Martin S Gould Sandra L DeMartino Julie A Siciliano Salvatore J Cascieri Margaret A Carella Anthony Carver Gwen Holmes Karen Schleif William A Danzeisen Renee Hazuda Daria Kessler Joseph Lineberger Janet Miller Michael Emini Emilio A |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. chris_lynch@merck.com |
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| 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. |
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