1,3,4-Trisubstituted Pyrrolidinones as Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists

Daniel L. Flynn; Clara I. Villamil; Daniel Becker; Gary W. Gullikson

doi:10.1016/S0960-894X(00)80224-3

1,3,4-Trisubstituted Pyrrolidinones as Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists

Daniel L. Flynn, Clara I. Villamil, Daniel Becker, Gary W. Gullikson

Department of Chemistry and Biochemistry

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

Abstract

A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar IC50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active.

Original language	American English
Journal	Chemistry: Faculty Publications and Other Works
Volume	2
Issue number	10
DOIs	https://doi.org/10.1016/S0960-894X(00)80224-3
State	Published - Oct 1 1992

Keywords

cholecystokinin antagonists
amino acids

Disciplines

Chemistry

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title = "1,3,4-Trisubstituted Pyrrolidinones as Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists",

abstract = " A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar IC50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active.",

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

year = "1992",

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T1 - 1,3,4-Trisubstituted Pyrrolidinones as Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists

AU - Flynn, Daniel L.

AU - Villamil, Clara I.

AU - Becker, Daniel

AU - Gullikson, Gary W.

PY - 1992/10/1

Y1 - 1992/10/1

N2 - A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar IC50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active.

AB - A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar IC50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active.

KW - cholecystokinin antagonists

KW - amino acids

UR - https://ecommons.luc.edu/chemistry_facpubs/6

U2 - 10.1016/S0960-894X(00)80224-3

DO - 10.1016/S0960-894X(00)80224-3

M3 - Article

VL - 2

JO - Chemistry: Faculty Publications and Other Works

JF - Chemistry: Faculty Publications and Other Works

IS - 10

ER -

1,3,4-Trisubstituted Pyrrolidinones as Scaffolds for Construction of Peptidomimetic Cholecystokinin Antagonists

Abstract

Keywords

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