1,2,3-triazolo[4,5-h]quinolines. III. Preparation and antimicrobial evaluation of 4-ethyl-4,7-dihydro-1(2)-R-1(2)H triazolo[4,5-h]quinolin-7-one-6-carboxylic acids as anti-infectives of the urinary tract.
Some 4-ethyl-1(2)-R-1(2)H-4,7-dihydro-triazolo[4,5-h]-quinolin-7-one-6- carboxylic acids were prepared as novel analogues of oxolinic acid, in order to discover the influence of the annelation position of the triazole ring on the antimicrobial activity that, in some isomers triazolo[4,5-f]quinoline carboxylic acids, is selective against Escherichia coli. Some interesting side reactions in the cyclization of 1(2)-R-1(2)H-benzotriazol-4-yl-aminomethylenemalonate are also described. The biological results indicate that this type of annelation is not profitable for antimicrobial activity.
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Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.
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D000892:Anti-Infective Agents, Urinary / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009268:Nalidixic Acid / Q000494:pharmacology; D010084:Oxidation-Reduction; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000892:Anti-Infective Agents, Urinary; D015363:Quinolones; D014230:Triazoles; C078324:4-ethyl-4,7-dihydrotriazolo(4,5-h)quinolin-7-one-6-carboxylic acid; D009268:Nalidixic Acid