Benzenesulphonylurea derivs.

摘要

Benzenesulphonylureas - where R = H, lower alkyl/Ph-alkyl - R1 = (2-8C)alkyl/alkenyl/HS-alkyl, (4-8C) alkoxyalkyl/alkyl-S-alkyl/a lkyl-SO-alkyl (at least 2 C as alkylene), lower Ph-alkyl, Ph-cyclopropyl, lower cyclohexylalkyl, cycloheptyl-Me/Et, cyclooctyl-Me, (1-2C)-endoalkylenecyclo-hexyl/hexenyl/hexyl-Me/hexeny l-Me, lower alkyl/alkoxy-cyclohexyl, (5-8C) cycloalkyl, cyclo-hexenyl/hexenyl-Me, heterocycle of 4-5C + 1 O/S and up to 2DELTA, same linked to N by CH2. - X = (1-6C)hydrocarbon chain, substd. by halo, OH, CO, lower alkoxy/acyloxy - Y = (1-4C) hydrocarbon chain - Z = H, lower alkyl/alkoxy/alkyl-S/alkyl-SO/alkyl-SO2/Ph-alkyl/acyl/ac yloxy/car- balkoxy/alkyl-carbamyl/dialkylcarbamyl, halo, (5-6C)cyclo-alkoxy, cyclohexyl, PhSO2, Ph, PhCO, CF3, OH, PhCH2O, COOH, CN, CONH2, NO2. - Z1,Z2 = H, lower alkyl/alkoxy or halo (Z being H, OH, COOH, alkyl, alkoxy or halo); Z1+Z2 = -OCH2O- (Z being H). - Hypoglycaemic agents. - Some of the cpds. show a lowering of the blood-sugar level in rabbits of 20-30% (3 hr.), following doses of 10 mg./kg. orally; the known antidiabetic, N-(p-tolysulphonyl)-N'-Bu urea, only shows an effect at 25 mg./kg. and above.