IMPROVEMENT OF THE ACTIVITY OF ANTIBACTERIAL AGENTS OF OXAZOLIDINONE BY ARGININE DERIVATIVES.

摘要

A product containing an oxazolidinone antibacterial agent and an arginine derivative, as a combined preparation for simultaneous, separate or sequential use to treat infections by gram-negative organisms in a mammal, the arginine derivative of formula A wherein R1 is a ) aryl, optionally substituted with C1-4 alkyl, C1-4 alkoxy, (C1-4) alkyl thio, halo or -NH2, b) - (CH2) i-aryl, in which aryl is substituted with C1-4 alkyl , C1-4 alkoxy, (C1-4) alkylthio, halo or - NH2, c) thienyl, furyl, pyridyl, benzofuranyl or benzothienyl; Z is R2 or -CHWR2; R2 is a) aryl, optionally substituted with one or two C1-4 alkyl, C1-4 alkoxy, (C1-4) alkyl thio, halo, -NH2, (C1-4) alkyl, amino (C1-4) alkyl or -NHOH, b) C1-4 alkyl, optionally substituted with fluoro, c) C1-4 alkoxy, d) (C1-4) alkylthio, e) halo, of) thienyl, furanyl or pyridyl; W is H, -NH2, alkyl (C1-4) amino, dialkyl (C1-4) amino, halo, hydroxy, C1-4 alkoxy, alkylthio or azaheterocycle; aryl is phenyl or naphthyl; Azaheterocycle is n-morpholinyl, n-piperazinyl, n-pyrrolidinyl, n-imidazolyl, n-pyrrolyl, n-pyrazolyl, n-triazolyl or n-tetrazolyl; and i is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.