Sugar A M, Liu X P
Evans Memorial Department of Clinical Research, Boston University Medical Center Hospital, MA 02118, USA.
Antimicrob Agents Chemother. 1996 May;40(5):1314-6. doi: 10.1128/AAC.40.5.1314.
The new triazole derivative SCH 56592 has been tested in a National Committee for Clinical Laboratory Standards-adapted in vitro susceptibility test, and its activity against 12 isolates of Blastomyces dermatitidis yeast-like forms has been compared with those of amphotericin B, itraconazole, and fluconazole. SCH 56592 was the most active of the four compounds, with an MIC at which 90% of the isolates are inhibited of 0.06 microgram/ml and a minimal fungicidal concentration at which 90% of the isolates are inhibited of 4 micrograms/ml. The results of the treatment of mice infected with B. dermatitidis with three different doses of SCH 56592 (25, 5, or 1 mg/kg of body weight), amphotericin B (1 mg/kg), or itraconazole (150 mg/kg) confirmed the potent activity of SCH 56592. Survival was prolonged at each dose of SCH 56592, and sterilization of the lungs occurred in the high-dose group but not in the groups treated with itraconazole or fluconazole. SCH 56592 is a promising new azole antifungal drug that should be studied in humans with blastomycosis.
新型三唑衍生物SCH 56592已在一项采用美国国家临床实验室标准委员会方法的体外药敏试验中进行了测试,并将其对12株皮炎芽生菌酵母样型的活性与两性霉素B、伊曲康唑和氟康唑进行了比较。SCH 56592是这四种化合物中活性最强的,其对90%分离株产生抑制作用的最低抑菌浓度为0.06微克/毫升,对90%分离株产生抑制作用的最低杀菌浓度为4微克/毫升。用三种不同剂量的SCH 56592(25、5或1毫克/千克体重)、两性霉素B(1毫克/千克)或伊曲康唑(150毫克/千克)治疗感染皮炎芽生菌的小鼠的结果证实了SCH 56592的强效活性。在每个SCH 56592剂量组中,小鼠存活期均延长,高剂量组肺部实现了菌清除,但伊曲康唑或氟康唑治疗组未实现。SCH 56592是一种有前景的新型唑类抗真菌药物,应在人类芽生菌病患者中进行研究。