|
|||||
|
|
Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents |
|
| Authors: | Harada Hiroshi Yamazaki Hiroshi Toyotomi Yoshihito Tateishi Hirotaka Mine Yukiko Yoshida Naoyuki Kato Shiro |
| Institution: | Medicinal Chemistry Group, Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki 33-94, Osaka 564-0053, Suita, Japan. |
| Abstract: | 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. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |