Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1, 2-a]pyrimidin-2-one derivatives. Issue 1 (1st January 2016)

• Record Type: Journal Article
• Authors: Silpa, Laurence; Niepceron, Alisson; Laurent, Fabrice; Brossier, Fabien; Pénichon, Mélanie; Enguehard-Gueiffier, Cécile; Abarbri, Mohamed; Silvestre, Anne; Petrignet, Julien
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 1(2016)
• Page Start: 114
• Page End: 120
• Publication Date: 2016-01-01
• Subjects: Pyrido[1, 2-a]pyrimidin-2-one -- Eimeria tenella -- Antiparasitic -- Anticoccidial activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.11.018
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 15 μM. 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.