Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
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DOI：
10.1016/j.bmcl.2005.04.060
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发表时间：
2005-07-01
影响因子：
2.7
通讯作者：
Wyvratt, M
中科院分区：
文献类型：
--
作者：
Biftu, T;Feng, D;Wyvratt, M
合成了几种2，3-二芳基吡咯类似物，并评价了其作为柔嫩艾美耳球虫cGMP依赖性蛋白激酶抑制剂的活性。体内抗球虫试验。4-氟苯基增强体外和体内活性。最有效的类似物是-5-（N-甲基、N-乙基和N-甲基氮杂环丁烷甲基）哌啶基衍生物12、23和34。这些化合物具有广谱活性。基于体内功效和合成成本，选择N-乙基类似物23作为用于田间试验的新型抗球虫剂。(c)2005爱思唯尔有限公司保留所有权利。
Several analogs of 2,3-diaryl pyrroles were synthesized and evaluated as inhibitors of Eimeria tenella cGMP-dependent protein kinase and in. in vivo anticoccidial assays. A 4-fluorophenyl group enhances both in vitro and in Vivo activities. The most potent analogs are the-5-(N-methyl, N-ethyl, and N-methylazetidine methyl) piperidyl derivatives 12, 23, and 34. These compounds have a broad spectrum of activity. Based on the in vivo efficacy and cost of synthesis, the N-ethyl analog 23 was chosen as a novel anticoccidial agent for a field trial. (c) 2005 Elsevier Ltd. All rights reserved.