title: Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2-a]pyrimidin-2-one derivatives.
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.
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Recherche et Innovation en Chimie Médicinale, Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 32 Avenue Monge, 37200 Tours, France; Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France.
authors.forename: Laurence
authors.initials: L
authors.lastname: Silpa
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France.
authors.forename: Alisson
authors.initials: A
authors.lastname: Niepceron
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France.
authors.forename: Fabrice
authors.initials: F
authors.lastname: Laurent
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France.
authors.forename: Fabien
authors.initials: F
authors.lastname: Brossier
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Recherche et Innovation en Chimie Médicinale, Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 32 Avenue Monge, 37200 Tours, France.
authors.forename: Mélanie
authors.initials: M
authors.lastname: Pénichon
authors.affiliation: UMR INSERM 1069 Nutrition, Croissance et Cancer, France.
authors.forename: Cécile
authors.initials: C
authors.lastname: Enguehard-Gueiffier
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Recherche et Innovation en Chimie Médicinale, Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 32 Avenue Monge, 37200 Tours, France.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Abarbri
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France.
authors.forename: Anne
authors.initials: A
authors.lastname: Silvestre
authors.affiliation: Laboratoire d'Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Recherche et Innovation en Chimie Médicinale, Université François Rabelais, Faculté des Sciences, Parc de Grandmont, 32 Avenue Monge, 37200 Tours, France.
authors.forename: Julien
authors.initials: J
authors.lastname: Petrignet
mesh_terms: D000818:Animals; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D003048:Coccidiosis / Q000188:drug therapy*; D003049:Coccidiostats / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D016786:Eimeria tenella / Q000187:drug effects*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D003049:Coccidiostats; D011728:Pyridones; D011744:Pyrimidinones
keywords: Anticoccidial activity; Antiparasitic; Eimeria tenella; Pyrido[1,2-a]pyrimidin-2-one