Alovero F, Nieto M, Mazzieri M R, Then R, Manzo R H
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Argentina.
Antimicrob Agents Chemother. 1998 Jun;42(6):1495-8. doi: 10.1128/AAC.42.6.1495.
The mode of action of sulfanilyl fluoroquinolones (NSFQs) was investigated with NSFQ-104, NSFQ-105, and some structurally related compounds. Evidence arising from interactions with p-aminobenzoic acid and trimethoprim suggested that a sulfonamidelike mechanism of action makes little or no contribution to the in vitro activity of NSFQs. NSFQ-105 showed an activity that inhibits gyrase-catalyzed DNA supercoiling that is similar to the activity of other fluoroquinolones. Also, NSFQ-105 uptake was decreased by the presence of Mg2+ and increased by a lower pH. These results indicate that NSFQs having only one ionizable group could exhibit more favorable kinetics of access to the bacterial cell than zwitterionic fluoroquinolones.
利用NSFQ - 104、NSFQ - 105以及一些结构相关的化合物对磺胺基氟喹诺酮类（NSFQs）的作用模式进行了研究。与对氨基苯甲酸和甲氧苄啶相互作用产生的证据表明，类似磺胺酰胺的作用机制对NSFQs的体外活性贡献很小或没有贡献。NSFQ - 105表现出抑制回旋酶催化的DNA超螺旋的活性，这与其他氟喹诺酮类的活性相似。此外，Mg2 +的存在会降低NSFQ - 105的摄取，而较低的pH值会增加其摄取。这些结果表明，与两性离子氟喹诺酮类相比，仅具有一个可电离基团的NSFQs在进入细菌细胞时可能表现出更有利的动力学。
