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

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

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.

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & Medicinal Chemistry Letters 2011-04, Vol.21 (8), p.2450-2455
Hauptverfasser: Skerlj, Renato, Bridger, Gary, Zhou, Yuanxi, Bourque, Elyse, Langille, Jonathan, Fluri, Maria Di, Bogucki, David, Yang, Wen, Wang, Letian, Nan, Susan, Baird, Ian, Metz, Markus, Darkes, Marilyn, Labrecque, Jean, Lau, Gloria, Fricker, Simon, Huskens, Dana, Schols, Dominique
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung: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.
ISSN:0960-894X