Acylureidoalkylphenylsulfonylureas with blood glucose lowering efficacy.

The structure and the synthesis of the blood-glucose lowering sulfonylurea glimepiride (Hoe 490) and of some analogues is described. The acylureido group of these compounds is prepared from lactams.

[Blood glucose-lowering acylaminoalkylbenzenesulfonamide derivatives with heterocyclic acyl residues].

The paper reports on acylaminoalkylbenzenesulfonamide derivatives with special heterocyclic acyl substituents. The compounds are characterized by an oxygen atom in ortho position to the carboxamide group of the heterocyclic acyl moiety. Several compounds show blood glucose lowering activities in animals similarly to glibenclamide.

[Synthesis of prednicarbate, an non-halogenated topical anti-inflammatory derivative of prednisolone-17-ethylcarbonate esters].

The synthesis of prednisolone-17-ethylcarbonate-21-propionate (5) (prednicarbate, Hoe 777) passing the intermediate products prednisolone-17,12-diethylorthocarbonate (2) and prednisolone-17-ethylcarbonate (3) as well as some physicochemical properties and spectroscopic data of (5), especially the 1H-NMR- and MS-spectrum, are reported. Prednicarbate has an optimal split of topical/systemic antiinflammatory activity.

Inhibition of 3H-glibenclamide binding to sulfonylurea receptors by oral antidiabetics.

Specific binding of 3H-glibenclamide (HB 419) is observed with membranes from rat cerebral cortex and rat beta-cell tumor. 3H-Glibenclamide binding is of high affinity, reversible, saturable, and can be displaced by oral antidiabetics of different structural types. Half maximal inhibition of binding correlates with the hypoglycemic action of the compounds.