Discovery of novel pyrazolo[1, 5-a]pyridine-based EP1 receptor antagonists by scaffold hopping: Design, synthesis, and structure-activity relationships. Issue 17 (1st September 2017)

• Record Type: Journal Article
• Authors: Nishigaya, Yosuke; Umei, Kentaro; Saito, Yoshifumi; Watanabe, Hiroyuki; Kondo, Tatsuhiro; Kondo, Atsushi; Kawamura, Naohiro; Tatani, Kazuya; Kohno, Yasushi; Tanaka, Nobuyuki; Seto, Shigeki
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 17(2017)
• Page Start: 4044
• Page End: 4050
• Publication Date: 2017-09-01
• Subjects: Scaffold-hopping -- Pyrazolo[1, 5-a]pyridine -- Structure-activity relationships -- EP1 antagonist; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.07.055
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A scaffold-hopping strategy towards a new pyrazolo[1, 5- a ]pyridine based core using molecular hybridization of two structurally distinct EP1 antagonists, followed by structure-activity relationship-guided optimization, resulted in the identification of potent EP1 antagonists exemplified by4c, 4f, and4j, which were shown to reduce pathological intravesical pressure in rats when administered at 1 mg/kg iv.