Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent
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- 作者：Jung Sang Parka ; b ; pjs2002@donga.co.kr" class="auth_mail" title="E-mail the corresponding author ; Weonbin Ima ; Sunghak Choia ; Sook Jin Parkb ; Jun Min Jungb ; Ki Seon Baekb ; Han Pyo Sonb ; Satyasheel Sharmab ; In Su Kimb ; Young Hoon Jungb ; yhjung@skku.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：5-HT4 ; hERG inhibition ; Gastric emptying rate ; Prokinetic ; GI disorder
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：75-88
- 全文大小：1220 K
文摘
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26 Novel benzamide derivatives of cisapride were synthesized as potential prokinetic agents.
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Alkyl piperidinyl moieties showed good binding affinities for the 5-HT4 receptor and low affinities for hERG.
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Compound 23g could be a good candidate to treat GI disorders, particularly functional dyspepsia.