两种新型氮杂索他汀衍生物GW471552和GW471558在两种免疫抑制大鼠模型中抗肺孢子虫病的治疗效果。
Therapeutic efficacies of GW471552 and GW471558, two new azasordarin derivatives, against pneumocystosis in two immunosuppressed-rat models.
作者信息
Jimenez Elena, Martínez Antonio, Aliouat El Moukhtar, Caballero Jesus, Dei-Cas Eduardo, Gargallo-Viola Domingo
机构信息
GlaxoSmithKline, Technological Park of Madrid, Severo Ochoa 2, 28760 Tres Cantos, Madrid., Spain.
出版信息
Antimicrob Agents Chemother. 2002 Aug;46(8):2648-50. doi: 10.1128/AAC.46.8.2648-2650.2002.
Abstract
Two new azasordarins, GW471552 and GW471558, were studied in vivo for treatment of Pneumocystis carinii pneumonia. In the Wistar rat spontaneous pneumonia model, both azasordarins significantly reduced the number of P. carinii cysts per gram of lung homogenate when administered at 1 mg/kg of body weight twice a day for 10 days. In a nude rat inoculation model, both compounds showed therapeutic efficacy at 0.25 mg/kg twice a day for 10 days.
摘要
对两种新型氮杂索德菌素GW471552和GW471558进行了治疗卡氏肺孢子虫肺炎的体内研究。在Wistar大鼠自发性肺炎模型中，当以1毫克/千克体重的剂量每日两次给药，持续10天时，两种氮杂索德菌素均显著降低了每克肺匀浆中卡氏肺孢子虫囊肿的数量。在裸鼠接种模型中，两种化合物在以0.25毫克/千克的剂量每日两次给药，持续10天时均显示出治疗效果。
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