1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

作者信息

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

机构信息

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

出版信息

Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23. doi: 10.1016/s0960-894x(02)00829-6.

DOI:10.1016/s0960-894x(02)00829-6

PMID:12467630

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.

摘要

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