Abstract:
Quinolne derivs. of formula (I) and their pharmaceutically acceptable salts are prepd.by condensing a pyridine deriv. of formula (II) and a quinoline carboxylic acid deriv. of formula (III) in the presence (or absence) of a solvent, at room temp. - 200 deg.C for 2-16 hrs. In the formulas, Z1, Z2 nd Z3 each = H, C1-3 alkyl, halogen, cyano, amino, hydroxy, C1-3 alkylamine or alkoxy; R1= ethyl or cyclopropyl; R2 and R3=H,F,Br or Cl; X=N, methyne or fluoromethyne, The cpds. (I) are useful as an antibacterial agent.
Abstract:
Benzoxazine carboxylic acid derivs. of formula (I) are new. In (I), R1-R5 each = H or lower alkyl; R6 and R7 each = H or C1-3 linear or cyclic lower alkyl, or substd. lower alkyl; the methyl gp. in the 3-position may be (S)-form or racemic form. Also claimed is the prepn. of (I) which comprises condensing a corresp. benzoxazine carboxylic acid deriv. of formula (II) with a 2,5- dihydropyrrole deriv. of formula (III) in the presence or absence of a solvent. Cpds. (I) have a good antibacterial activity and broad spectrum antibacterial action against Gram positive and Gram negative bacteria.
Abstract:
Quinolone derivs. of formula (I) and, when R1 is H, their acid addn. salts and hydrates are new. Z = halo or NH2; R1 = H or a cation. R2 = H, lower alkyl or formyl; m = 1-3; n = 1 or 2. Also claimed is the prepn. of (I) which comprises e.g. condensing corresp. quinolone deriv. with a leaving gp. in the 10-position with a diazabicycloamine. (I) may be orally or parenterally administered at a dose of 0.1-1.5 (0.2-0.8) g/kay to a 60 kg adult. Cpds. (I) are used for the treatment of bacterial infections. (I) have a better and wider range of activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) also have a good antibacterial activity against methicillin resistant bacteria.