Amine-constrained pyridazinone histamine H 3 receptor antagonists

…, T Bailey, E Bacon, L Aimone, Z Huang, J Lyons…

Index: Sundar, Babu G.; Bailey, Thomas; Bacon, Edward; Aimone, Lisa; Huang, Zeqi; Lyons, Jacquelyn; Raddatz, Rita; Hudkins, Robert Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5543 - 5546

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Citation Number: 13

Abstract

Pyridazinone 1 was recently reported as a potent H3R antagonist with good drug-like properties and in vivo activity. A series of constrained amine analogs of 1 was synthesized to identify compounds with improved pharmacokinetic profiles. From these efforts, a new class of (S)-2-pyrrolidin-1-ylmethyl-1-pyrrolidinyl amides was identified.