Moxifloxacin HCl

Moxifloxacin HCl（莫西沙星盐酸）是具有广谱抗菌活性的抗感染化合物[1]。

Moxifloxacin是第四代氟喹诺酮类抗菌剂，抗菌谱广，可以抗革兰氏阳性菌和革兰氏阴性菌[1]。Moxifloxacin的抗菌活性主要通过抑制DNA拓扑异构酶II和拓扑异构酶IV的活性，这两个拓扑异构酶参与细菌DNA的复制、转录、重组和修复[2]。Moxifloxacin的口服生物利用度可以高达90％。由于moxifloxacin不是肝细胞色素P-450同功酶系统的抑制剂或底物，所以它没有潜在的药物相互作用。Moxifloxacin有约90-97％的细菌清除率和88-97％的临床成功率。Ciprofloxacin（环丙沙星）敏感株中，Moxifloxacin的MIC90s小于等于 0.6 μg/mL。肠球菌中moxifloxacin的MIC90s范围为1至4 μg/mL。副流感嗜血杆菌中moxifloxacin的MIC90s从0.03到0.125 μg/ mL。其它细菌中moxifloxacin的MIC90s为4 μg/mL。脆弱拟杆菌中moxifloxacin的MIC90s为0.25-4 μg/mL[3]。

Moxifloxacin也抑制hPON1（人血清对氧磷酶-1）的酶活性，Ki值为2.641 ± 0.004 mM[4]。

参考文献：?
[1].?? ?Cruz LA, Hall R: Enantiomeric purity assay of moxifloxacin hydrochloride by capillary electrophoresis. J Pharm Biomed Anal 2005, 38(1):8-13.
[2].?? ?Kamruzzaman M, Alam AM, Lee SH, Ragupathy D, Kim YH, Park SR, Kim SH: Spectrofluorimetric study of the interaction between europium(III) and moxifloxacin in micellar solution and its analytical application. Spectrochim Acta A Mol Biomol Spectrosc 2012, 86:375-380.
[3].?? ?Culley CM, Lacy MK, Klutman N, Edwards B: Moxifloxacin: clinical efficacy and safety. Am J Health Syst Pharm 2001, 58(5):379-388.
[4].?? ?Turkes C, Soyut H, Beydemir S: Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium. J Enzyme Inhib Med Chem 2014:1-7