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. 2016 Jan 1;26(1):114-20.
doi: 10.1016/j.bmcl.2015.11.018. Epub 2015 Nov 10.

Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2-a]pyrimidin-2-one derivatives

Laurence Silpa  1 , Alisson Niepceron  2 , Fabrice Laurent  2 , Fabien Brossier  2 , Mélanie Pénichon  3 , Cécile Enguehard-Gueiffier  4 , Mohamed Abarbri  3 , Anne Silvestre  2 , Julien Petrignet  3
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Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2-a]pyrimidin-2-one derivatives

Laurence Silpa et al. Bioorg Med Chem Lett. .

Abstract

Screening 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 MDBK cell invasion in vitro than the lead compound.

Keywords: Anticoccidial activity; Antiparasitic; Eimeria tenella; Pyrido[1,2-a]pyrimidin-2-one.

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