title: Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
abstract: 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.
authors.affiliation: Genzyme Corp., 153 Second Avenue, Waltham, MA 02451, USA. renato.skerlj@genzyme.com
authors.forename: Renato
authors.initials: R
authors.lastname: Skerlj
authors.forename: Gary
authors.initials: G
authors.lastname: Bridger
authors.forename: Yuanxi
authors.initials: Y
authors.lastname: Zhou
authors.forename: Elyse
authors.initials: E
authors.lastname: Bourque
authors.forename: Jonathan
authors.initials: J
authors.lastname: Langille
authors.forename: Maria
authors.initials: M
authors.lastname: Di Fluri
authors.forename: David
authors.initials: D
authors.lastname: Bogucki
authors.forename: Wen
authors.initials: W
authors.lastname: Yang
authors.forename: Tongshuang
authors.initials: T
authors.lastname: Li
authors.forename: Letian
authors.initials: L
authors.lastname: Wang
authors.forename: Susan
authors.initials: S
authors.lastname: Nan
authors.forename: Ian
authors.initials: I
authors.lastname: Baird
authors.forename: Markus
authors.initials: M
authors.lastname: Metz
authors.forename: Marilyn
authors.initials: M
authors.lastname: Darkes
authors.forename: Jean
authors.initials: J
authors.lastname: Labrecque
authors.forename: Gloria
authors.initials: G
authors.lastname: Lau
authors.forename: Simon
authors.initials: S
authors.lastname: Fricker
authors.forename: Dana
authors.initials: D
authors.lastname: Huskens
authors.forename: Dominique
authors.initials: D
authors.lastname: Schols
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D065100:CCR5 Receptor Antagonists; D003497:Cyclic N-Oxides / Q000737:chemistry*; D004285:Dogs; D015195:Drug Design; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D010091:Oximes; D010880:Piperidines / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000577:Amides; D065100:CCR5 Receptor Antagonists; D003497:Cyclic N-Oxides; D010091:Oximes; D010880:Piperidines; D011725:Pyridines; D019713:Receptors, CCR5; C438583:Ancriviroc