| 摘要 |
FIELD: organic synthesis and biologically-active compounds. SUBSTANCE: invention provides new beta-lactam derivatives with general formula I: beta (I) wherein Z is methylene, oxygen, or sulfur and R is hydrogen or lower alkyl optionally substituted by lower alkoxycarbonyl, carbamoyl, lower cycloalkylcarbamoyl, phenylcarbamoyl, or hydroxyphenylcarbamoyl; lower alkenylmethyl; formyl; lower alkanoyl and alkylsulfonyl both optionally substituted by halogen, cyan, or carbamoyl-lower-alkylthio group; carbamoyl optionally substituted by lower cycloalkyl, lower- alkoxycabonyl-lower-alkyl, benzyloxycarbonyl-lower-alkyl, or carboxy- lower-alkyl; or annular structure with general formulas Q-X-CO- (a1) or Q-X-SO<SB>2</SB> constituting 5- or 6-membered rings optionally including nitrogen, sulfur, and/or oxygen and X is <EMI ID=0.500 HE=15 WI=84 TI=CHI> and A is lower alkyl, hydroxy-lower-alkyl, vinyl, cyanovinyl, lower alkoxy, optionally phenyl- substituted lower alkylsulfonyloxy, -S-Het or -S-CH<SB>2</SB>-Het residues in which Het is 5- or 6-membered nitrogen- and/or sulfur-containing cycle and L lower alkanoyloxy, lower carbamoyloxy, lower alkoxycarbonyl, carboxy, azido, lower alkanoylamino, lower alkylsulfonylamino, 6-membered ring linked to nitrogen atom, S-Het or -CH<SB>2</SB>-L residues; or their pharmaceutically acceptable, easily hydrolysible esters and salts. Products show beta-lactamase inhibition activity and are useful in combating beta-lactamase- producing pathogenic organisms in combination with beta-lactam antibiotics. Products can also be used individually in treating infection diseases. EFFECT: increased choice of pharmaceutically active compounds. 42 cl, 2 dwg, 5 tbl, 109 ex
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