abstract |
The invention relates to naphthyridine-, quinoline- or benzoxazine-carboxylic acid derivatives, in particular the compounds (I) of the general formula YC CH C - C (O) -C-C (O) OR ,, z6 x-C-CH-g -sn (I) where T. is RI; N-CCP5 X × MCH.); (СН2) .- 1СНг. I - “C CH -Cn-CH2, or / (W-7 Cr5Kb, p CCHoJ V ssng) / (c); le-: o-ny - u); s (b)); X - CH; CC1; CF, N, C-OH; C O - C, alkyl; p 1,2,3 or 4; , 2,3 or 4, and p + n. in the amount of 2.3.4 or.; five; p 0.1 or 2; n 1 or 2 .; i R, H; , Rj Н, СН or R Н, С-С-alkyl, С + Hydroxy-alkyl, trifluoroethyl, at Rj I С, -С4-alkyl or С, -С-alkoxy-; or C —C3 alkyl when, and Z is the value of a, with n + n 3; or CjHj; R4 C-C-alkyl, C2-C4-hydroxyalkyl, trifluoroethyl alkyl, or C-C-alkyl, when X C-OH in which hydrogen and R in the NR group can be mixed with a ring-forming radical - CHRg- CHRj, where or C, -C j-alkyl; or C-Pd-alkyl, or their pharmaceutically acceptable salts with antibacterial properties. The goal is to obtain more active compounds of the above class. The synthesis of compounds (I) is carried out by treating the corresponding chlorine or fluorine-substituted naphthyridinecarboxylic or quinolinecarboxylic acid with the corresponding amine. Compounds of compound (I) are reduced either in free form or in the form of an acid addition salt. Tests of compounds (I) show that they have a high antibacterial activity with a minimally used concentration of 0.1 µg / ml, which allows reducing the therapeutic dose for the organism. 3 tab. S W with G5 O SL 00 4 CM |