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  • Title: Synthesis of 7-thio-substituted 4-oxoquinoline-3-carboxylic acids with antibacterial activity.
    Author: Nishimura Y, Hirose T, Okada H, Shibamori K, Nakano J, Matsumoto J.
    Journal: Chem Pharm Bull (Tokyo); 1990 Aug; 38(8):2190-6. PubMed ID: 2126225.
    Abstract:
    A series of C-7 thio-substituted 1-cyclopropyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared and tested for their antibacterial activity. Structure-activity relationships associated with the C-5 and C-7 substituents were discussed. Among the C-7 substituents including alkylthio, arylthio, heteroarylthio, and cyclic aminothio groups, a 2-aminoethylthio group was the best for enhancing in vitro antibacterial activity. The C-5 variants increased activity in the order OH less than F less than H less than NH2. Of compounds prepared in this work, 5-amino-7-(2-aminoethyl)thio-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4 -oxo-quinoline-3-carboxylic acid (18) was the most active.
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