Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2- a ]pyrimidin-2-one derivatives
作者: Laurence SilpaAlisson NiepceronFabrice LaurentFabien BrossierMélanie PénichonCécile Enguehard-GueiffierMohamed AbarbriAnne SilvestreJulien Petrignet
作者单位: 1Laboratoire 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
2Laboratoire d’Infectiologie et Santé Publique (UMR Université François Rabelais/INRA 1282), Equipe Apicomplexes et Immunité Mucosale INRA, UMR1282, F-37380 Nouzilly, France
3UMR INSERM 1069 Nutrition, Croissance et Cancer, France
刊名: Bioorganic & Medicinal Chemistry Letters, 2016, Vol.26 (1), pp.114-120
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2015.11.018
关键词: Pyrido[12- a ]pyrimidin-2-oneEimeria tenellaAntiparasiticAnticoccidial activity
英文摘要: Abstract(#br)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 IC 50 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.
全文获取路径: Elsevier  (合作)
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影响因子:2.338 (2012)

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