新型取代苯并恶唑并喹唑啉酮类作为强效抗精神病和抗惊厥药物。
Newer substituted benzoxazepinyl-quinazolinones as potent antipsychotic and anticonvulsant agents.
作者信息
Bajaj Kiran, Srivastava Virendra Kishor, Kumar Ashok
机构信息
Medicinal Chemistry Division, Department of Pharmacology, Lala Lajpat Rai Memorial Medical College, Meerut, U.P., India.
出版信息
Arzneimittelforschung. 2003;53(7):480-5. doi: 10.1055/s-0031-1297137.
3-Amino-[2'-substitutedaryl-3'-substitutedarylaminomethylene-2',3'- dihydro-1',5'-benzoxazepin-4'-yl]-2-methyl-quinazolin-4(3H)-ones 11-18 and 3-amino-[2'-substituted aryl-3'-substitutedaryl-azo-2',3'- dihydro-1',5'-benzoxazepin-4'-yl]-2-methyl-quinazolin-4(3H)-ones 19-26 were synthesized from 3-amino-[2'-substitutedaryl-2',3'-dihydro-1',5'- benzoxazepin-4'-yl]-2-methyl-quinazolin-4(3H)-ones 7-10 by Mannich's reaction and by diazotisation, respectively, on the 3rd position of the benzoxazepine ring of the compounds 7-10. The newly synthesized compounds showed potent antipsychotic and anticonvulsant activities.
3-氨基-[2'-取代芳基-3'-取代芳氨基亚甲基-2',3'-二氢-1',5'-苯并二氮杂䓬-4'-基]-2-甲基喹唑啉-4(3H)-酮11 - 18以及3-氨基-[2'-取代芳基-3'-取代芳基偶氮-2',3'-二氢-1',5'-苯并二氮杂䓬-4'-基]-2-甲基喹唑啉-4(3H)-酮19 - 26分别通过曼尼希反应以及重氮化反应，由3-氨基-[2'-取代芳基-2',3'-二氢-1',5'-苯并二氮杂䓬-4'-基]-2-甲基喹唑啉-4(3H)-酮7 - 10在化合物7 - 10的苯并二氮杂䓬环的第3位合成得到。新合成的化合物显示出强效的抗精神病和抗惊厥活性。
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