A series of novel 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity were synthesized in this study. These derivatives were evaluated for their in vitro activity against some mycobacteria. All of the synthesized compounds were less active than the parent 8-OCH(3) ciprofloxacin against Mycobacteriumsmegmatis CMCC 93202, but most of the methylene isatin derivatives were more active than 8-OCH(3) ciprofloxacin, ciprofloxacin, isoniazid and rifampin against MTB H37Rv ATCC 27294. It was noted that compound 3b (MIC: 0.074 μM) was 2-13 fold more potent than the reference compounds against MTB H37Rv ATCC 27294, and compounds 3f and 3i-k (MIC: 6.72-7.05 μM) were around 1.6 fold more potent than the parent 8-OCH(3) ciprofloxacin, 3.5 fold more potent than ciprofloxacin against MDR-MTB 09710.
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Reduced phototoxicity of a fluoroquinolone antibacterial agent with a methoxy group at the 8 position in mice irradiated with long-wavelength UV light.
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Toxicology Research Laboratories, Chugai Pharmaceutical Co. Ltd., Nagano, Japan.
A newly developed fluoroquinoline, Q-35 (8-OCH3), in which a methoxy group was substituted at the 8 position of the quinoline nucleus, was very stable under irradiation with long-wave UV light (UVA). Derivatives, a fluoroquinolone with no substitution (the 8-H analog) and one in which a fluorine was substituted (the 8-F analog), were degraded in their solutions by the UVA irradiation. The phototoxic inducibility by these derivatives was further studied in a murine model.
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