Discovery of novel pyrazolo[1,5-a]pyridine-based EP 1 receptor antagonists by scaffold hopping: Design, synthesis, and structure-activity relationships

A scaffold-hopping strategy towards a new pyrazolo[1,5-a]pyridine based core using molecular hybridization of two structurally distinct EP antagonists, followed by structure-activity relationship-guided optimization, resulted in the identification of potent EP antagonists exemplified by 4c, 4f, and...

Ausführliche Beschreibung

Bibliographische Detailangaben

Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-09, Vol.27 (17), p.4044
Hauptverfasser:	Nishigaya, Yosuke, Umei, Kentaro, Saito, Yoshifumi, Watanabe, Hiroyuki, Kondo, Tatsuhiro, Kondo, Atsushi, Kawamura, Naohiro, Tatani, Kazuya, Kohno, Yasushi, Tanaka, Nobuyuki, Seto, Shigeki
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Dose-Response Relationship, Drug Drug Discovery Molecular Structure Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Rats Receptors, Prostaglandin E, EP1 Subtype - antagonists & inhibitors Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!