Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2-a]pyrimidin-2-one derivatives
作者:Laurence Silpa、Alisson Niepceron、Fabrice Laurent、Fabien Brossier、Mélanie Pénichon、Cécile Enguehard-Gueiffier、Mohamed Abarbri、Anne Silvestre、Julien Petrignet
DOI:10.1016/j.bmcl.2015.11.018
日期:2016.1
of our chemical library to discover new molecules exhibiting in vitro activity against the invasion of host cells by Eimeria tenella revealed a lead compound with an IC50 of 15μM. Structure-activity relationship studies were conducted with 34 newly synthesized compounds to identify more active molecules and enhance in vitro activity against the parasite. Four compounds were more effective in inhibiting
筛选我们的化学文库以发现表现出抗艾美尔球虫侵袭宿主细胞的体外活性的新分子,发现了一种铅化合物,IC50为15μM。使用34种新合成的化合物进行了结构-活性关系研究,以鉴定更多活性分子并增强体外抗寄生虫活性。四种化合物在体外抑制MDBK细胞入侵方面比先导化合物更有效。