title: Pyridothiadiazinedioxides structurally related to quinazolinones cholecystokinin/gastrin receptor ligands: synthesis and biological evaluation.
abstract: The synthesis of 3-aralkyl-4-aryl-4H-, 3-aralkylamino-4-aryl-4H- and 3-aralkylsulfanyl-4-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1, 1-dioxides is described. Moreover, the affinity of the different compounds towards the cholecystokinin CCK-A and CCK-B receptors was evaluated. For selected compounds, affinity on the two receptor subtypes was expressed in the micromolar range. This was comparable to the affinity observed with the naturally occurring CCK receptor antagonist asperlicin.
authors.affiliation: Laboratoire de Chimie Pharmaceutique, Institut de Pharmacie, Université de Liège, 3, rue Fusch, B-4000 Liège, Belgium.
authors.forename: B
authors.initials: B
authors.lastname: Pirotte
authors.forename: P
authors.initials: P
authors.lastname: de Tullio
authors.forename: T
authors.initials: T
authors.lastname: Podona
authors.forename: O
authors.initials: O
authors.lastname: Diouf
authors.forename: D
authors.initials: D
authors.lastname: Dewalque
authors.forename: P
authors.initials: P
authors.lastname: Neven
authors.forename: B
authors.initials: B
authors.lastname: Masereel
authors.forename: D H
authors.initials: DH
authors.lastname: Caignard P
authors.forename: P
authors.initials: P
authors.lastname: Renard
authors.forename: J
authors.initials: J
authors.lastname: Delarge
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D007700:Kinetics; D008024:Ligands; D008297:Male; D011799:Quinazolines / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000378:metabolism*; D012844:Sincalide / Q000378:metabolism; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D008024:Ligands; D011799:Quinazolines; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; D013829:Thiadiazines; D012844:Sincalide