Synthesis and SAR of 5-Amino- and 5-(Aminomethyl)benzofuran Histamine H3 Receptor Antagonists with Improved Potency

A new series of H3 receptor antagonists was discovered with nanomolar and subnanomolar affinities at human and rat H3 receptors. Starting from an earlier, more structurally limited series of benzofurans, the present series of compounds demonstrated increased structural variety and flexibility with g...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-10, Vol.48 (20), p.6482-6490
Hauptverfasser:	Sun, Minghua, Zhao, Chen, Gfesser, Gregory A, Thiffault, Christine, Miller, Thomas R, Marsh, Kennan, Wetter, Jill, Curtis, Michael, Faghih, Ramin, Esbenshade, Timothy A, Hancock, Arthur A, Cowart, Marlon
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzofurans - chemical synthesis Benzofurans - pharmacokinetics Benzofurans - pharmacology Biological and medical sciences Cells, Cultured Hepatocytes - drug effects Hepatocytes - metabolism Histamine Antagonists - chemical synthesis Histamine Antagonists - pharmacokinetics Histamine Antagonists - pharmacology Humans Male Medical sciences Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Phospholipids - biosynthesis Pyrrolidines - chemical synthesis Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology Radioligand Assay Rats Rats, Sprague-Dawley Receptors, Histamine H3 - drug effects Receptors, Histamine H3 - metabolism Structure-Activity Relationship
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