Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists

Autor:	Kennan C. Marsh, Wesley J. Dwight, Arthur A. Hancock, Jill M. McVey, Jia Bao Pan, Ramin Faghih, Kathy M. Krueger, Youssef L. Bennani, Gerard B. Fox, Timothy A. Esbenshade
Rok vydání:	2003
Předmět:	Magnetic Resonance Spectroscopy medicine.drug_class Stereochemistry Clinical Biochemistry Histamine Antagonists Drinking Behavior Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Mass Spectrometry Mice Radioligand Assay Structure-Activity Relationship Histamine receptor Dogs Receptors Biogenic Amine In vivo Drug Discovery medicine Animals Humans Receptors Histamine H3 Amines Cloning Molecular Receptor Molecular Biology Chromatography High Pressure Liquid Cerebral Cortex Dose-Response Relationship Drug Chemistry Organic Chemistry Antagonist Haplorhini Amides In vitro Rats Molecular Medicine Histamine H3 receptor
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:1325-1328
ISSN:	0960-894X
Popis:	Novel 4′-[(NR1R2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H 3 receptors. Most compounds were highly potent and selective for human and rat H 3 receptors and selected examples such as A-349821 showed functional antagonism of H 3 receptors in vitro and in a mouse dipsogenia model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a320ca39430445fdcf92976a2bd7854 https://doi.org/10.1016/s0960-894x(03)00118-5 Zobrazit plný text záznamu Full Text from ScienceDirect