FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to synthetic biologically active substances of heterocyclic series, possessing antimicrobial activity and represents products of modification of known β-lactam antibiotic - ampicillin, including all spatial isomers of claimed substance, all their tautomeric and salt forms. Antomicrobial substance with general formula: , where R is selected from group: H, methyl, ethyl, n-alkyl (C3-C9), phenyl; X1 and X3 are selected from group: CH2, O or N (NH or NR, where R - methyl, ethyl, linear or branched alkyl, alkenyl or cycloalkyl C3-C10, CH2CH2OEt, CH2CH2CH2OMe, Ph, benzole derivative, substituted one or several times with linear or branched alkyl, alkenyl or cycloalkyl C1-C9, halogen (F, O or Br), CF3, methoxy group or other alkoxy group, carboxyl or carboxyalkyl, or simultaneously by several of said substituents, CH2Ph, CH2CH2Ph, CH(CH3)Ph, CH2C6H4(OMe-p), CH2C6H4(F-p), CH2CH2C6H4(F-p), CH2CH2C6H3(3,4-diOMe); 2-furylmethyl, 2-(2-thienyl)ethyl; X2 is selected from group: C=0, C=S, CH2, CMe2, C(C5H10-cyclo).
EFFECT: invention provides biologically active substance with high antibacterial activity and wide spectrum of action, efficiently influencing bacteria, present in human cells and in composition of biofilms.
11 tbl, 12 ex
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Authors
Dates
2011-09-10—Published
2010-08-06—Filed