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

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

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Cell Survival / drug effects
  • Coccidiosis / drug therapy*
  • Coccidiostats / chemical synthesis*
  • Coccidiostats / chemistry
  • Coccidiostats / pharmacology*
  • Dose-Response Relationship, Drug
  • Eimeria tenella / drug effects*
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Pyridones / chemical synthesis
  • Pyridones / chemistry
  • Pyridones / pharmacology*
  • Pyrimidinones / chemical synthesis
  • Pyrimidinones / chemistry
  • Pyrimidinones / pharmacology*
  • Structure-Activity Relationship

Substances

  • Coccidiostats
  • Pyridones
  • Pyrimidinones