| Autor: |
Freidinger RM; Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486., Whitter WL, Gould NP, Holloway MK, Chang RS, Lotti VJ |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1990 Feb; Vol. 33 (2), pp. 591-5. |
| DOI: |
10.1021/jm00164a020 |
| Abstrakt: |
Novel aryl amide analogues of glutamic acid dialkylamide have been synthesized to test for a possible structural analogy between glutamic acid and benzodiazepine CCK antagonists such as compounds 2 and 24 (lorglumide and MK-329, respectively). In support of the structural model, certain of these hybrid compounds are more potent in pancreas CCK radioligand binding assays than corresponding lorglumide-type reference compounds. Modifications previously found in the benzodiazepine antagonists to result in brain CCK/gastrin receptor selectivity were also incorporated to produce an aryl urea series of glutamic acid analogues. None of these compounds were brain CCK/gastrin selective; however, one was potent and selective in the pancreas binding assay. The model appears to be most useful in the design of selective ligands for the pancreas type CCK receptor. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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