强效咪唑并吡啶抗球虫剂的合成及构效关系研究
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.
作者信息
Liang Gui-Bai, Qian Xiaoxia, Feng Dennis, Fisher Michael, Brown Christine M, Gurnett Anne, Leavitt Penny Sue, Liberator Paul A, Misura Andrew S, Tamas Tamas, Schmatz Dennis M, Wyvratt Matthew, Biftu Tesfaye
机构信息
Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3558-61. doi: 10.1016/j.bmcl.2007.04.041. Epub 2007 Apr 24.
Diaryl imidazo[1,2-a]pyridine derivatives, such as 6a and 7i, have been synthesized and found to be potent inhibitors of parasite PKG activity. The most potent compounds are the 7-isopropylaminomethyl analog 6a and 2-isopropylamino analog 7i. These compounds are also fully active in in vivo assay as anticoccidial agents at 25 ppm in feed.
二芳基咪唑并[1,2 - a]吡啶衍生物，如6a和7i，已被合成并发现是寄生虫蛋白激酶G（PKG）活性的有效抑制剂。最有效的化合物是7 - 异丙基氨基甲基类似物6a和2 - 异丙基氨基类似物7i。这些化合物在饲料中以25 ppm作为抗球虫剂在体内试验中也具有完全活性。
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