1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists
| Autor: | Daniel L. Flynn, Chafiq Moummi, Dai-Chang Yang, Daniel P. Becker, G. W. Gullikson, Clara I. Villamil |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
chemistry.chemical_classification
Peptidomimetic Stereochemistry digestive oral and skin physiology Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Combinatorial chemistry In vitro Amino acid Orally active chemistry Competitive antagonist Drug Discovery Molecular Medicine Pyrrolidinones Molecular Biology hormones hormone substitutes and hormone antagonists Cholecystokinin |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 2:1251-1256 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)80224-3 |
| Popis: | 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 IC 50 values in a CCK-A receptor binding assay. Compound 1E behaves as a competitive antagonist in vitro and is orally active. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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