Novel N-[1-(1-substituted 4-piperidinylmethyl)-4piperidinyl]benzamides as potent colonic prokinetic agents

A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT(4) receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-ch...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-03, Vol.12 (6), p.967-970
Hauptverfasser:	HARADA, Hiroshi, YAMAZAKI, Hiroshi, TOYOTOMI, Yoshihito, TATEISHI, Hirotaka, MINE, Yukiko, YOSHIDA, Naoyuki, KATO, Shiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzamides - administration & dosage Benzamides - chemical synthesis Benzamides - pharmacology Biological and medical sciences Digestive system Digestive System - drug effects Dogs Gastrointestinal Agents - administration & dosage Gastrointestinal Agents - chemical synthesis Gastrointestinal Agents - pharmacology Medical sciences Pharmacology. Drug treatments Protein Binding Serotonin - metabolism Serotonin Receptor Agonists - administration & dosage Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - pharmacology Structure-Activity Relationship
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Zusammenfassung:	A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT(4) receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-chloro-2-methoxybenzamide (15) was found to have a potent binding affinity for 5-HT(4) receptors (IC(50): 6.47nM) and showed excellent colonic prokinetic activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00060-4