BICYCLIC DERIVATIVES OF 1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXYLIC ACID OR THEIR SALTS AND PHARMACEUTICAL COMPOSITION SHOWING ANTIBACTERIAL ACTIVITY

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to bicyclic derivatives of 1,4-dihydro-4-oxoquinoline-3-carboxylic acid of the formula (I) where X and X - halide atom; A is a group ; X - hydrogen, halide or alkyl; R - hydrogen or ethoxycarbonyl; R is H or amino-group; R - bicyclic h...

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Hauptverfasser: MAKOTO TAKEMURA, JUITI KIMURA, NORIKAZU MATSUKHASI
Format: Patent
Sprache:eng
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Zusammenfassung:FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to bicyclic derivatives of 1,4-dihydro-4-oxoquinoline-3-carboxylic acid of the formula (I) where X and X - halide atom; A is a group ; X - hydrogen, halide or alkyl; R - hydrogen or ethoxycarbonyl; R is H or amino-group; R - bicyclic heterocyclic substituent of the formula (A) R where R and - hydrogen or taken together they form a bond; Y is R where C2-5 - H or -CH2--acyl; Z - oxygen atom or ; m and n are a whole numbers from 0 to 2 independently being m + n = 2-3; p, q and r - are whole numbers from 0 to 3 and their sum a whole number from 0 to 3. Invention proposes a pharmaceutical composition containing a compound of the formula (I) as an active component that shows antibacterial activity. EFFECT: improved method of synthesis, enhanced antibacterial activity of compounds. 25 cl, 1 tbl, 42 ex