Literature DB >> 26597537

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

Laurence Silpa1, Alisson Niepceron2, Fabrice Laurent2, Fabien Brossier2, Mélanie Pénichon3, Cécile Enguehard-Gueiffier4, Mohamed Abarbri3, Anne Silvestre2, Julien Petrignet3.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

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Substances：

Year:  2015        PMID： 26597537     DOI： 10.1016/j.bmcl.2015.11.018

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Hexafluoroisopropanol mediated benign synthesis of 2H-pyrido[1,2-a]pyrimidin-2-ones by using a domino protocol.

Authors:  Zakeyah Alsharif; Mohamad Akbar Ali; Hessa Alkhattabi; Derika Jones; Evan Delancey; P C Ravikumar; Mohammad A Alam
Journal:  New J Chem       Date:  2017-10-20       Impact factor: 3.591

2.  Efficient microwave-assisted Suzuki-Miyaura cross-coupling reaction of 3-bromo pyrazolo[1,5-a]pyrimidin-5(4H)-one: towards a new access to 3,5-diarylated 7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine derivatives.

Authors:  Badr Jismy; Gérald Guillaumet; Mohamed Akssira; Abdellatif Tikad; Mohamed Abarbri
Journal:  RSC Adv       Date:  2021-01-04       Impact factor: 4.036

3.  Simple and Expedient Access to Novel Fluorinated Thiazolo- and Oxazolo[3,2-a]pyrimidin-7-one Derivatives and Their Functionalization via Palladium-Catalyzed Reactions.

Authors:  Wafa Blancou; Badr Jismy; Soufiane Touil; Hassan Allouchi; Mohamed Abarbri
Journal:  Molecules       Date:  2022-05-07       Impact factor: 4.927

4.  Efficient Access to 3,5-Disubstituted 7-(Trifluoromethyl)pyrazolo[1,5-a]pyrimidines Involving SNAr and Suzuki Cross-Coupling Reactions.

Authors:  Badr Jismy; Abdellatif Tikad; Mohamed Akssira; Gérald Guillaumet; Mohamed Abarbri
Journal:  Molecules       Date:  2020-04-28       Impact factor: 4.411
  4 in total

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