Dicationic furans inhibit development of Cryptosporidium parvum in HSD/ICR suckling Swiss mice
Dicationic furans inhibit development of Cryptosporidium parvum in HSD/ICR suckling Swiss mice
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DOI：
10.2307/3284603
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发表时间：
1998-08-01
影响因子：
1.3
通讯作者：
Tidwell, RR
中科院分区：
文献类型：
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作者：
Blagburn, BL;Drain, KL;Tidwell, RR
通过乳鼠模型评价双阳离子二芳基呋喃对微小隐孢子虫的功效。将候选药物溶解或悬浮在去离子水中，并在第0-5天（处理第0天）以恒定剂量率经口给予实验接种了梭菌卵囊的ICR Swiss乳鼠。小的效力基于从第6天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处理小鼠中回收的卵囊数量。化合物1、2、4和9显示上级对C.小的化合物3、5、6、7、8、11、17、18和19也显著减少了从处理的小鼠中回收的卵囊的数量，但表现出对照的17 - 65%的功效。化合物4对C.在剂量低至8.5毫克/公斤体重的parvum。化合物4被鉴定为用于在其他动物模型中进行额外研究的先导化合物。
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.