Ram Vishnu Ji, Tripathi Brajendra K, Srivastava Arvind K
Division of Medicinal Chemistry, Central Drug Research Institute, 226001, Lucknow, India.
Bioorg Med Chem. 2003 May 29;11(11):2439-44. doi: 10.1016/s0968-0896(03)00142-1.
A series of 2-sec-amino-3H-quinazolin-4-ones (4a-p) and 4-sec-amino-2-chloroquinazolines (5a-b) have been synthesized by nucleophilic substitution reaction of 2-chloro-4(3H)-quinazolones (3) and 2,4-dichloroquinazolines (2) with amines, respectively. Most of the synthesized compounds were evaluated for antihyperglycemic activity but only 4a,b,d,j,o displayed significant reduction in blood glucose level in streptozotocin and sucrose loaded rat models.
通过2-氯-4(3H)-喹唑啉酮(3)和2,4-二氯喹唑啉(2)分别与胺的亲核取代反应,合成了一系列2-氨基-3H-喹唑啉-4-酮(4a-p)和4-氨基-2-氯喹唑啉(5a-b)。对大多数合成化合物进行了抗高血糖活性评估,但只有4a、b、d、j、o在链脲佐菌素和蔗糖负荷大鼠模型中显示出血糖水平显著降低。