Amine-constrained pyridazinone histamine H3 receptor antagonists

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-09, Vol.21 (18), p.5543-5546
Hauptverfasser:	Sundar, Babu G., Bailey, Thomas, Bacon, Edward, Aimone, Lisa, Huang, Zeqi, Lyons, Jacquelyn, Raddatz, Rita, Hudkins, Robert
Format:	Artikel
Sprache:	eng
Schlagworte:	amides Amines - chemistry Animals antagonists Biological and medical sciences chemistry Dose-Response Relationship, Drug H3R antagonist histamine Histamine H3 Antagonists - chemical synthesis Histamine H3 Antagonists - chemistry Histamine H3 Antagonists - pharmacology Humans Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors pharmacokinetics Pharmacology. Drug treatments Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Pyridazinone Rat PK Rats Receptors, Histamine H3 - metabolism Serotoninergic system Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.06.094