| abstract |
Peperidine derivs. of formula (I) are new: (R1 = H, branched, linear or cyclic, opt. unsatd., aliphatic hydrocarbyl, aryl or heterocyclyl, all opt. substd.; R2 = H, OH, OR', SH, SR', NH2, NHR', NR'R", NH2CH2, R'NHCH2, R'R"NCH2, COOH, COOR', HOCH2, R'CONHCH2, R'CONR"CH2, R'SO2NHCH2, R'SO2NR"CH2, R'NHCONHCH2, R'NHCSNHCH2, R'OCONHCH2, SO3H, CN, CONH2, CONHR' or CONR'R"; R3 can be as R1 but is pref H, CH3, CH2OH, CH2NH2, CH2NHR', CH2NR'R", R'CONH.CH2, R'CONR"CH2, HalCH2, R'OCH2, R'COOCH2, R'SO2OCH2, R'SO2NHCH2, R'NH.CONHCH2, R'NHCSNH.CH2, R'OCONHCH2, CN, COOH, COOR', CONH2, CONHR', R'SO2NR"CH2, CONR'R"; R' and R" are as for R1; when (i) R3 = CH2OH; R2 = H or OH; (ii) R3 = CH2NH2 and R2 = OH; and also (iii) when R3=H, R2=H, OH, SO3H, CN or CH2NH2, R1 cannot be H). (I) inhibit alpha-glucosidases, esp. disaccharidases, so are useful in treating pre-diabetes, gastritis, obstipation, caries, gastro-intestinal infections, meterorism, flatulence, hypertension, atherosclerosis and esp. adiposity, diabetes and hyperlipoproteinaemia. They are also useful as animal feed additives to improve the meat-fat distribution. |