Effect of 1-[4- [2-(4-bromobenzenesulfonamino) ethyl] phenylsulfonyl]-3-(trans-4-methylcyclohexyl)urea (I4), a new synthetic sulfonylurea compound, on glucose metabolism in vivo and in vitro.

Background: 1-[4-[2-(4-Bromobenzenesulfonamino)ethyl]phenylsulfonyl]-3-(trans-4-methylcyclohexyl)urea (I4, CAS 865483-06-3), a totally synthetic new sulfonylurea compound, incorporating part of the hypoglycemic structure of glimepiride (CAS 93479-97-1) and having anti-TXA2 receptor properties, was designed and synthesized. Its hypoglycemic property had not been reported yet.

Aim: To study the hypoglycemic effects of I4 and its primary mechanisms of action.

[Design, synthesis and hypoglycemic activity of alpha-benzylsuccinic acid derivatives].

Based on the SAR of glinide agents, mitiglinide has been modified to study the SAR of glinides. a-Benzylsuccinic acid derivatives which were designed and synthesized in order to find some more hypoglycemic active agents and further investigate the SAR of this class of compounds. From ethyl succinate and substituded benzaldehydes, twelve new target compounds were synthesized by codensation, hydrolysis, anhydridization, amidation and hydrogenization reactions, and their hypoglycemic activity were evaluated with glucose oxidase kit.

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.