Quinazolinone derivatives: synthesis and binding evaluation on cholecystokinin receptors.
A series of 2-methyl-3-amino-4(H)-quinazolinone and of 2-phenyl-3-amino-4(H)-quinazolinone derivatives were synthesized and examined for their CCK receptor affinities. These compounds displayed micromolar affinities for CCK-B rather than CCK-A receptor and the obtained results confirm that the 4(3H)-quinazolinone nucleous represent a useful template for the development of selective CCK-B receptor ligands.
Varnavas
A
A
Dipartimento di Scienze Farmaceutiche, Università di Trieste, Italy.
Lassiani
L
L
Luxich
E
E
Zacchigna
M
M
Boccù
E
E
D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D010179:Pancreas / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011949:Receptors, Cholecystokinin / Q000187:drug effects / Q000378:metabolism*; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
D011799:Quinazolines; D011949:Receptors, Cholecystokinin