[Synthesis of potential CCK antagonist quinazolone derivatives].
An original route has been found for the synthesis of [1,4]diazepino-quinazolones, a new ring system of heterocondensed quinazolones. These anthranilicacid-alanin-beta-alanin cyclopeptide derivatives constitute a structural moiety of asperlicin, the first natural cholecystokinin antagonist alkaloid. These compounds are therefore potential CCK antagonists. The new compounds were prepared via condensation of 2-amino-alkyl-quinazolones, obtained from 2-alkyl-quinazolones by side-chain substitution, with 1,3-bifunctional-reagents. We studied the cyclisation process under basic, acidic and phase-transfer catalyzed conditions. The structures of the synthesized compounds were characterized by IR, UV and NMR spectroscopy.
Szabó
M
M
Semmelweis Orvostudományi Egyetem, Gyógyszerészi Kémiai Intézet, Budapest.
Kökösi
J
J
Orfi
L
L
D002766:Cholecystokinin / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013053:Spectrophotometry; D013329:Structure-Activity Relationship
D011799:Quinazolines; D002766:Cholecystokinin
Potenciális CCK-antagonista kinazolon-származékok szintézise.