摘要
艾沙康唑是一种三唑类广谱抗真菌药,该药以水溶性前药硫酸艾沙康唑鎓的形式静脉注射或口服给药,它能通过抑制真菌细胞色素P45014DM的生物功能干扰其细胞壁的形成,最终达到抗真菌的作用。本文综述艾沙康唑、水溶性侧链结构片段及硫酸艾沙康唑鎓的合成方法,并对合成路线的优缺点进行评述,为硫酸艾沙康唑鎓工艺的开发奠定基础。
Isavuconazole is a broad-spectrum triazole antifungal agent,which is administered as a water-soluble prodrug-isavuconazonium sulfate. Recently,its oral and intravenous formulations are available. Isavuconazole inhibits fungal cytochrome P45014 DM,thus interferes with the biological function of cell wall formation and plays the antifungal role. In this paper,we summarize the synthetic methods of isavuconazole,water-soluble segments of side chain and isavuconazonium sulfate and evaluate their advantages and disadvantages,which lays a foundation for isavuconazonium sulfate technology development.
引文
[1]Mccormack PL.Isavuconazonium:first global approval[J].Drugs,2015,75(7):817-822.
[2]宋婷婷,冯婧劼,马荣.抗真菌药物艾莎康唑研究进展[J].中国新药杂志,2015,24(3):288-297.
[3]栾升霖.艾沙康唑硫酸酯(Isavuconazonium sulfate)[J].中国药物化学杂志,2015,25(5):414.
[4]US FDA.FDA Approves new antifungal drug Cresemba[EB/OL](2015-03-06)[2016-01-05].http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm437106.htm.
[5]Saratosa MS.Process for the manufacture of enantiomerically pure antifungal azoles as ravuconazole and isavuconazole:US,20110087030[P].2001-04-14.
[6]Chigasaki TH,Kawasaki SI,Chigasaki YI,et al.Azoles for treatment of fungal infections:US,006300353[P].2001-10-09.
[7]Soukup M.Intermediate halophenyl derivatives and their use in a process for preparing azole derivatives:US,20040176432[P].2004-09-09.
[8]福田宽,早濑忠胜,水口荣作,等.N-取代的氨基甲酰氧基烷基-吡咯鎓衍生物:CN,1387529A,[P].2002-12-25.
[9]Ohwada J,Tsukazaki M,Hayase T,et al.Design,synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole[J].Bioorg Med Chem Lett,2003,13(2):191-196.
[10]石建.三唑类抗真菌药物研究新进展[J].国外医药抗生素分册,1998,19(2):135-139.
[11]向道春,饶子超,刘东.三唑类抗真菌药物的研究进展[J].医药导报,2009,28:56-58.
[12]任晓慧,周有骏,陈新,等.深部真菌感染及其治疗药物研究现状[J].武汉工业学院学报,2012,31(1):22-31.
[13]Marisa H,Carol A.Isavuconazole:a new broad-spectrum triazoleantifungal agent[J].Clin Infect Dis,2015,61(9):1-8.
