Benzotriazonine as a new core structure for the design of CCK-receptor antagonists.
The search for heterocyclic scaffolds for the design of non-peptidic and highly selective agonists or antagonists of peptide hormone receptors led to 4-N-benzyl-2,3,4,5,6,7-hexahydro-1H-1,4,7-benzotriazonin-2, 6-dione with a 9-membered core structure as a new low mass lead compound that exhibits submicromolar antagonistic activity at the CCK-A receptor with a 54-fold selectivity over the CCK-B/gastrin receptor.
D000818:Animals; D016466:CHO Cells / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D006224:Cricetinae; D003460:Crystallization; D015195:Drug Design; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism