Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

Autor:	Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Jonathan Langille, Maria Di Fluri, David Bogucki, Wen Yang, Tongshuang Li, Letian Wang, Susan Nan, Ian Baird, Markus Metz, Marilyn Darkes, Jean Labrecque, Gloria Lau, Simon Fricker, Dana Huskens, Dominique Schols
Rok vydání:	2011
Předmět:	Receptors CCR5 Pyridines Organic Chemistry Clinical Biochemistry Pharmaceutical Science Virus Replication Amides Biochemistry Rats Cyclic N-Oxides Structure-Activity Relationship Dogs Piperidines Drug Design CCR5 Receptor Antagonists Oximes Drug Discovery HIV-1 Animals Humans Molecular Medicine Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:2450-2455
ISSN:	0960-894X
Popis:	A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db65c2f32206af093539db4b4c1cf2c1 https://doi.org/10.1016/j.bmcl.2011.02.058 Zobrazit plný text záznamu Full Text from ScienceDirect