Blagburn B L, Drain K L, Land T M, Moore P H, Kinard R G, Lindsay D S, Kumar A, Shi J, Boykin D W, Tidwell R R
Department of Pathobiology, College of Veterinary Medicine, Auburn University, Alabama 36849-5519, USA.
J Parasitol. 1998 Aug;84(4):851-6.
The efficacy of dicationic diarylfurans was evaluated against Cryptosporidium parvum by a suckling murine model. Candidate drugs were solubilized or suspended in deionized water and administered orally at a constant dose rate on days 0-5 (treatment day 0) to suckling ICR Swiss mice experimentally inoculated with oocysts of C. parvum. Efficacy was based on numbers of oocysts recovered from the intestinal tracts of mice subjected to necropsy examination on day 6. Numerous candidate furans significantly reduced the numbers of oocysts recovered from treated mice compared with control mice. Compounds 1, 2, 4, and 9 demonstrated superior efficacies (10% of controls or better) against C. parvum. Compounds 3, 5, 6, 7, 8, 11, 17, 18, and 19 also significantly reduced the numbers of oocysts recovered from treated mice but demonstrated efficacies ranging from 17 to 65% of controls. Compound 4 was particularly efficacious against C. parvum at a dosage as low as 8.5 mg/kg of body weight. Compound 4 is identified as a lead compound for additional studies in other animal models.
通过乳鼠模型评估了双阳离子二芳基呋喃对微小隐孢子虫的疗效。候选药物用去离子水溶解或悬浮，并于第0 - 5天（治疗第0天）以恒定剂量率口服给予经实验接种微小隐孢子虫卵囊的ICR瑞士乳鼠。疗效基于第6天对进行尸检的小鼠肠道中回收的卵囊数量。与对照小鼠相比，许多候选呋喃显著减少了从治疗小鼠中回收的卵囊数量。化合物1、2、4和9对微小隐孢子虫显示出优异的疗效（为对照的10%或更低）。化合物3、5、6、7、8、11、17、18和19也显著减少了从治疗小鼠中回收的卵囊数量，但疗效为对照的17%至65%。化合物4在低至8.5 mg/kg体重的剂量下对微小隐孢子虫特别有效。化合物4被确定为在其他动物模型中进行进一步研究的先导化合物。
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