Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.
作者信息
Becker Daniel P, Flynn Daniel L, Villamil Clara I
机构信息
Department of Medicinal Chemistry, Pfizer Research and Development, 4901 Searle Parkway, Skokie, IL 60077, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jun 21;14(12):3073-5. doi: 10.1016/j.bmcl.2004.04.021.
PMID:15149647
Abstract
Pyrrolizidine benzamide (+/-)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT(4) agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (+/-)-2 has an EC(50) of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.
摘要
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