Synthesis and antihyperglycemic activity of suitably functionalized 3H-quinazolin-4-ones.
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.
Ram
Vishnu Ji
VJ
Division of Medicinal Chemistry, Central Drug Research Institute, 226001, Lucknow, India. vjiram@yahoo.com
Farhanullah
Tripathi
Brajendra K
BK
Srivastava
Arvind K
AK
D000818:Animals; D019540:Area Under Curve; D001786:Blood Glucose / Q000378:metabolism; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology*; D008297:Male; D011799:Quinazolines / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013311:Streptozocin; D013329:Structure-Activity Relationship
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D011799:Quinazolines; D013311:Streptozocin