Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H 3 receptor antagonists

NC Becknell, JA Lyons, LD Aimone, JA Gruner…

Index: Becknell, Nadine C.; Lyons, Jacquelyn A.; Aimone, Lisa D.; Gruner, John A.; Mathiasen, Joanne R.; Raddatz, Rita; Hudkins, Robert L. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 23 p. 7076 - 7080

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Citation Number: 12

Abstract

6-{4-[3-(R)-2-Methylpyrrolidin-1-yl) propoxy]-phenyl}-2H-pyridazin-3-one 6 (Irdabisant; CEP- 26401) was recently reported as a potent H3R antagonist with excellent drug-like properties and in vivo activity that advanced into clinical evaluation. A series of pyridone analogs of 6 ...