Details

Autor(en) / Beteiligte

• Nishigaya, Yosuke
• Umei, Kentaro
• Saito, Yoshifumi
• Watanabe, Hiroyuki
• Kondo, Tatsuhiro
• Kondo, Atsushi
• Kawamura, Naohiro
• Tatani, Kazuya
• Kohno, Yasushi
• Tanaka, Nobuyuki
• Seto, Shigeki

Titel

Discovery of novel pyrazolo[1,5-a]pyridine-based EP1 receptor antagonists by scaffold hopping: Design, synthesis, and structure-activity relationships

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2017-09, Vol.27 (17), p.4044-4050

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2017

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• [Display omitted] 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 by 4c, 4f, and 4j, which were shown to reduce pathological intravesical pressure in rats when administered at 1mg/kg iv.