title: Synthesis and biological evaluation of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups as potential hypoglycemic agents.
abstract: 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.
authors.affiliation: Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
authors.forename: Hui-Bin
authors.initials: HB
authors.lastname: Zhang
authors.forename: Ya-An
authors.initials: YA
authors.lastname: Zhang
authors.forename: Guan-Zhong
authors.initials: GZ
authors.lastname: Wu
authors.forename: Jin-Pei
authors.initials: JP
authors.lastname: Zhou
authors.forename: Wen-Long
authors.initials: WL
authors.lastname: Huang
authors.forename: Xiao-Wen
authors.initials: XW
authors.lastname: Hu
mesh_terms: 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
chemical_list: D005947:Glucose; D007004:Hypoglycemic Agents; D013449:Sulfonamides; D013453:Sulfonylurea Compounds; D013890:Thiourea; D000096926:Benzenesulfonamides