Holmes D H, Ensminger P W, Gordee R S
Antimicrob Agents Chemother. 1974 Oct;6(4):432-6. doi: 10.1128/AAC.6.4.432.
The antimicrobial activity of cinoxacin, 1-ethyl-4(1H)-oxo-[1,3]dioxolo[4,5-g]cinnoline-3-carboxylic acid, previously reported as compound 64716, was determined and compared with other antimicrobial agents at a dosage of 12 mg/kg once daily in a descending pyelonephritis rat model with Escherichia coli and Proteus mirabilis as infecting organisms. Cinoxacin was considerably more effective than either nalidixic acid or oxolinic acid when all three were administered orally at 3 mg/kg four times daily. The presence of demonstrable serum activity with a high recovery in urine indicates cinoxacin possesses highly desirable properties of an effective oral chemotherapeutic agent for urinary tract infections.
西诺沙星,即1-乙基-4(1H)-氧代-[1,3]二氧杂环戊烯并[4,5-g]喹啉-3-羧酸,先前报道为化合物64716,其抗菌活性在以大肠杆菌和奇异变形杆菌作为感染菌的下行性肾盂肾炎大鼠模型中进行了测定,并与其他抗菌剂进行了比较,给药剂量为每日一次12mg/kg。当三种药物均以每日4次、每次3mg/kg口服给药时,西诺沙星比萘啶酸或奥索利酸的效果显著更好。可证明的血清活性以及尿液中的高回收率表明,西诺沙星具有作为尿路感染有效口服化疗药物的非常理想的特性。