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

Document Type

Article

Publication Date

10-1-1992

Publication Title

Bioorganic & Medicinal Chemistry Letters

Volume

2

Issue

10

Pages

1251-1256

Publisher Name

Elsevier

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.

Comments

Author Posting © Elsevier, 1992. The definitive version was published in Bioorganic & Medicinal Chemistry Letters, Volume 2, Issue 10, October 1992. http://dx.doi.org/10.1016/S0960-894X(00)80224-3

Creative Commons License

Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.

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