Bridgehead-methyl Analog of SC-53116 as a 5-HT4 Agonist

Daniel Becker; Daniel L. Flynn; Clara I. Villamil

doi:10.1016/j.bmcl.2004.04.021

Bridgehead-methyl Analog of SC-53116 as a 5-HT4 Agonist

Daniel Becker, Daniel L. Flynn, Clara I. Villamil

Department of Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

Abstract

Pyrrolizidine benzamide (±)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (±)-2 has an EC50 of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.

Original language	American English
Journal	Chemistry: Faculty Publications and Other Works
Volume	14
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2004.04.021
State	Published - Jun 21 2004

Keywords

bridgehead-methyl analog

Disciplines

Chemistry

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title = "Bridgehead-methyl Analog of SC-53116 as a 5-HT4 Agonist",

abstract = " Pyrrolizidine benzamide (±)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (±)-2 has an EC50 of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.",

keywords = "bridgehead-methyl analog",

author = "Daniel Becker and Flynn, {Daniel L.} and Villamil, {Clara I.}",

year = "2004",

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AU - Flynn, Daniel L.

AU - Villamil, Clara I.

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N2 - Pyrrolizidine benzamide (±)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (±)-2 has an EC50 of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.

AB - Pyrrolizidine benzamide (±)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (±)-2 has an EC50 of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.

KW - bridgehead-methyl analog

UR - https://ecommons.luc.edu/chemistry_facpubs/21

U2 - 10.1016/j.bmcl.2004.04.021

DO - 10.1016/j.bmcl.2004.04.021

M3 - Article

VL - 14

JO - Chemistry: Faculty Publications and Other Works

JF - Chemistry: Faculty Publications and Other Works

IS - 12

ER -

Bridgehead-methyl Analog of SC-53116 as a 5-HT4 Agonist

Abstract

Keywords

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