Pfaller M A, Messer S, Jones R N
Department of Pathology, University of Iowa College of Medicine, Iowa City 52242, USA.
Antimicrob Agents Chemother. 1997 Feb;41(2):233-5. doi: 10.1128/AAC.41.2.233.
Sch 56592 is a new triazole agent with potent, broad-spectrum antifungal activity. The in vitro activities of Sch 56592, itraconazole, fluconazole, amphotericin B, and flucytosine (5-FC) against 404 clinical isolates of Candida spp. (382 isolates) and Saccharomyces cerevisiae (22 isolates) were investigated. In vitro susceptibility testing was performed by a broth microdilution method performed according to National Committee for Clinical Laboratory Standards guidelines. Overall, Sch 56592 was very active (MIC at which 90% of isolates are inhibited [MIC90], 0.5 microgram/ml) against these yeast isolates. Sch 56592 was most active against Candida tropicalis, Candida parapsilosis, candida lusitaniae, and Candida stellatoidea (MIC90, < or = 0.12 microgram/ml) and was least active against Candida glabrata (MIC90, 2.0 micrograms/ml). Sch 56592 was 2- to 32-fold more active than amphotericin B and 5-FC against all species except C. glabrata. By comparison with the other triazoles, Sch 56592 was equivalent to itraconazole and greater than or equal to eightfold more active than fluconazole. On the basis of these results, Sch 56592 has promising antifungal activity, and further in vitro and in vivo investigations are warranted.
Sch 56592是一种新型三唑类药物,具有强效、广谱抗真菌活性。研究了Sch 56592、伊曲康唑、氟康唑、两性霉素B和氟胞嘧啶(5-FC)对404株念珠菌属临床分离株(382株)和酿酒酵母(22株)的体外活性。体外药敏试验采用肉汤微量稀释法,按照美国国家临床实验室标准委员会的指南进行。总体而言,Sch 56592对这些酵母分离株具有很强的活性(90%分离株被抑制时的最低抑菌浓度[MIC90]为0.5微克/毫升)。Sch 56592对热带念珠菌、近平滑念珠菌、葡萄牙念珠菌和星状念珠菌活性最强(MIC90,≤0.12微克/毫升),对光滑念珠菌活性最弱(MIC90,2.0微克/毫升)。除光滑念珠菌外,Sch 56592对所有菌种的活性比两性霉素B和5-FC高2至32倍。与其他三唑类药物相比,Sch 56592与伊曲康唑相当,比氟康唑活性高8倍以上。基于这些结果,Sch 56592具有良好的抗真菌活性,有必要进一步进行体外和体内研究。