Marco F, Pfaller M A, Messer S A, Jones R N
Department of Pathology, University of Iowa College of Medicine, Iowa City 52242, USA.
Mycopathologia. 1998;141(2):73-7. doi: 10.1023/a:1006970503053.
Sch 56592 is a new triazole derivative that possesses potent, broad-spectrum antifungal activity. We evaluated the in vitro activity of Sch 56592 compared with that of itraconazole, amphotericin B and 5-fluorocytosine against 51 clinical isolates of filamentous fungi, including Aspergillus flavus (10), A. fumigatus (12), Fusarium spp. (13), Rhizopus spp. (6), Pseudallescheria boydii (5), and one isolate each of Acremonium spp., A. niger, A. terreus, Paecilomyces spp., and Trichoderma spp. In vitro susceptibility testing was performed using the microdilution broth method outlined in the NCCLS 27-A document. Sch 56592 was highly active against A. flavus (MIC90, 0.25 micrograms/ml), A. fumigatus (MIC90, 0.12 micrograms/ml), P. boydii (MIC50, 1 microgram/ml) and Rhizopus spp (MIC50, 1 microgram/ml). By comparison with itraconazole, Sch 56592 was four-to eight-fold more active against isolates of Aspergillus and both compounds showed equipotent in vitro activity against P. boydii and Rhizopus spp. Sch 56592 was four- to 16-fold more active than amphotericin B against Aspergillus spp. and P. boydii and both antifungal drugs displayed similar activity against Rhizopus spp. Overall, Sch 56592 showed good in vitro activity against all isolates tested (MIC, < or = 2 micrograms/ml) except isolates of Fusarium (MIC range, (1-->4 micrograms/ml). On the basis of these data Sch 56592 has promising activity against Aspergillus spp. and other species of filamentous fungi that are likely to be encountered clinically. Additional in vitro and in vivo studies are warranted.
Sch 56592是一种新型三唑衍生物,具有强大的广谱抗真菌活性。我们评估了Sch 56592与伊曲康唑、两性霉素B和5-氟胞嘧啶相比,对51株丝状真菌临床分离株的体外活性,这些分离株包括黄曲霉(10株)、烟曲霉(12株)、镰刀菌属(13株)、根霉属(6株)、波氏假阿利什霉(5株),以及顶孢霉属、黑曲霉、土曲霉、拟青霉属和木霉属各1株分离株。使用NCCLS 27-A文件中概述的微量稀释肉汤法进行体外药敏试验。Sch 56592对黄曲霉(MIC90,0.25微克/毫升)、烟曲霉(MIC90,0.12微克/毫升)、波氏假阿利什霉(MIC50,1微克/毫升)和根霉属(MIC50,1微克/毫升)具有高度活性。与伊曲康唑相比,Sch 56592对曲霉分离株的活性高4至8倍,且两种化合物对波氏假阿利什霉和根霉属显示出同等的体外活性。Sch 56592对曲霉属和波氏假阿利什霉的活性比两性霉素B高4至16倍,且两种抗真菌药物对根霉属显示出相似的活性。总体而言,Sch 56592对除镰刀菌分离株(MIC范围,(1→4微克/毫升)之外的所有测试分离株均显示出良好的体外活性(MIC,≤2微克/毫升)。基于这些数据,Sch 56592对曲霉属和其他临床上可能遇到的丝状真菌具有有前景的活性。有必要进行额外的体外和体内研究。