Synthesis and biological evaluation of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups as potential hypoglycemic agents.
A novel class of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups were designed and synthesized. The target compounds were assayed for the effects on the insulin release of isolated rat pancreatic islets and the glucose transport in adipocytes of rats. Some of them exhibited high potency. Compound 10 also had potent antiplatelet activity and showed an excellent property to protect collagen-epinephrine-induced mice mortality as well as plasma glucose-lowering activity in vivo. The preliminary pharmacological profile of compound 10 showed that it might be useful in the treatment of diabetics with cardiovascular and nephropathy complications.
Zhang
Hui-Bin
HB
Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
Zhang
Ya-An
YA
Wu
Guan-Zhong
GZ
Zhou
Jin-Pei
JP
Huang
Wen-Long
WL
Hu
Xiao-Wen
XW
D017667:Adipocytes / Q000378:metabolism; D000818:Animals; D001692:Biological Transport; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003920:Diabetes Mellitus / Q000188:drug therapy; D015195:Drug Design; D005947:Glucose / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007515:Islets of Langerhans / Q000166:cytology; D008954:Models, Biological; D008956:Models, Chemical; D051381:Rats; D013449:Sulfonamides / Q000737:chemistry*; D013453:Sulfonylurea Compounds / Q000737:chemistry*; D013890:Thiourea / Q000737:chemistry*; D000096926:Benzenesulfonamides
D005947:Glucose; D007004:Hypoglycemic Agents; D013449:Sulfonamides; D013453:Sulfonylurea Compounds; D013890:Thiourea; D000096926:Benzenesulfonamides