Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3073-5. doi: 10.1016/j.bmcl.2004.04.021.
Daniel P Becker  1 ,  Daniel L Flynn ,  Clara I Villamil
Affiliations
  • 1. Department of Medicinal Chemistry, Pfizer Research and Development, 4901 Searle Parkway, Skokie, IL 60077, USA. [email protected]
PMID: 15149647 DOI: 10.1016/j.bmcl.2004.04.021
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.

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