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

Autor:	Christopher L. Lynch, Janet Lineberger, Julie A. DeMartino, Ping Chen, Scott C. Berk, Margaret A. Cascieri, Gwen Carver, Michael W. Miller, Edward J. Holson, Liya Chen, Martin S. Springer, Sandra L. Gould, Kevin T. Chapman, Jeffrey J. Hale, Karen Holmes, Renee Danzeisen, William A. Schleif, Malcolm MacCoss, Joseph Kessler, Richard J. Budhu, Anthony Carella, Charles G. Caldwell, Christopher A. Willoughby, Lorraine Malkowitz, Daria J. Hazuda, Sander G. Mills, Salvatore J. Siciliano, Emilio A. Emini, Amy Gentry, Keith G. Rosauer
Rok vydání:	2002
Předmět:	Pyrrolidines Stereochemistry Anti-HIV Agents Metabolic Clearance Rate Clinical Biochemistry Pharmaceutical Science CCR5 receptor antagonist Biochemistry Chemical synthesis Pyrrolidine Sulfone chemistry.chemical_compound Radioligand Assay Structure-Activity Relationship Dogs Piperidines Drug Discovery Tumor Cells Cultured Moiety Animals Humans Methylene Molecular Biology Organic Chemistry Antagonist Macaca mulatta Rats chemistry CCR5 Receptor Antagonists Leukocytes Mononuclear Molecular Medicine Piperidine Half-Life
Zdroj:	Bioorganicmedicinal chemistry letters. 13(1)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fd06eeeda03c2b2b0bcbdb849fb5f96 https://pubmed.ncbi.nlm.nih.gov/12467630 Zobrazit plný text záznamu Full Text from ScienceDirect