Development of 1,4-benzodiazepine cholecystokinin type B antagonists
| Autor: | M G, Bock, R M, DiPardo, B E, Evans, K E, Rittle, W L, Whitter, V M, Garsky, K F, Gilbert, J L, Leighton, K L, Carson, E C, Mellin |
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| Rok vydání: | 1993 |
| Předmět: |
medicine.drug_class
Guinea Pigs Neuropeptide Biological Availability Pharmacology Peptide hormone digestive system Cholecystokinin receptor Devazepide Sincalide Benzodiazepines Structure-Activity Relationship Drug Discovery medicine Animals Receptor Pancreas Cholecystokinin Cerebral Cortex Benzodiazepine Benzodiazepinones Molecular Structure Chemistry Phenylurea Compounds digestive oral and skin physiology Antagonist Rats Gastrointestinal hormone Molecular Medicine Receptors Cholecystokinin hormones hormone substitutes and hormone antagonists |
| Zdroj: | Journal of medicinal chemistry. 36(26) |
| ISSN: | 0022-2623 |
| Popis: | A series of 3-(arylureido)-5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin (CCK), are described. Derived by reasoned modification of the CCK-A selective 3-carboxamido-1,4-benzodiazepine, MK-329, this paper chronicles the development of potent, orally effective compounds in which selectivity for the CCK-B receptor subtype was achieved. The principal lead structure that emerged from these studied is L-365,260, a compound which has been submitted for clinical evaluation. Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK-B receptor affinity and selectivity of this class of compounds. |
| Databáze: | OpenAIRE |
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