SCH 39304及其异构体RR 42427和SS 42426用于治疗小鼠隐球菌性和球孢子菌性脑膜炎的比较。
Comparison of SCH 39304 and its isomers, RR 42427 and SS 42426, for treatment of murine cryptococcal and coccidioidal meningitis.
作者信息
Allendoerfer R, Yates R R, Marquis A J, Loebenberg D, Rinaldi M G, Graybill J R
机构信息
Department of Medicine, University of Texas Health Science Center, San Antonio.
出版信息
Antimicrob Agents Chemother. 1992 Jan;36(1):217-9. doi: 10.1128/AAC.36.1.217.
SCH 39304 (304) and its isomers, SCH 42426 (426) and SCH 42427 (427), are new orally administered antifungal azole derivatives. In this study, we compared the efficacy of 304 with that of 426 and 427 in murine models of cryptococcal and coccidioidal meningitis. On day 18 postinfection with Cryptococcus neoformans, controls showed 80% mortality. The 50% protective doses calculated at this day were 0.56 mg of 304 per kg of body weight, 23.5 mg of 426 per kg, and 0.11 mg of 427 per kg. Controls with coccidioidal meningitis all succumbed, and treated mice at the same time point showed 50% protective doses of 10.8 mg/kg for 304, 200 mg/kg for 426, and 2.1 mg/kg for 427. We conclude that isomer 427 is five times as potent, whereas 426 is 1/50th as potent as 304 in these experimental mycoses.
SCH 39304（304）及其异构体SCH 42426（426）和SCH 42427（427）是新型口服抗真菌唑类衍生物。在本研究中，我们在隐球菌性和球孢子菌性脑膜炎的小鼠模型中比较了304与426和427的疗效。在感染新型隐球菌后的第18天，对照组的死亡率为80%。在这一天计算出的50%保护剂量分别为：304每千克体重0.56毫克，426每千克23.5毫克，427每千克0.11毫克。患有球孢子菌性脑膜炎的对照组全部死亡，在同一时间点接受治疗的小鼠中，304的50%保护剂量为10.8毫克/千克，426为200毫克/千克，427为2.1毫克/千克。我们得出结论，在这些实验性真菌病中，异构体427的效力是304的五倍，而426的效力是304的1/50。
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