Literature DB >> 16517161

Synthesis and SAR studies of diarylpyrrole anticoccidial agents.

Xiaoxia Qian1, Gui-Bai Liang, Dennis Feng, Michael Fisher, Tami Crumley, Sandra Rattray, Paula M Dulski, Anne Gurnett, Penny Sue Leavitt, Paul A Liberator, Andrew S Misura, Samantha Samaras, Tamas Tamas, Dennis M Schmatz, Matthew Wyvratt, Tesfaye Biftu.   

Abstract

2-(4-Fluorophenyl)-3-(4-pyridinyl)-5-substituted pyrroles were prepared and evaluated as anticoccidial agents in both in vitro and in vivo assays. Among the compounds evaluated, the dimethylamine-substituted pyrrole 19a is the most potent inhibitor of Eimeria tenella PKG (cGMP-dependent protein kinase). Further SAR studies on the side chain of the 2-pyrrolidine nitrogen did not enhance in vivo anticoccidial activity.

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Year:  2006        PMID: 16517161     DOI: 10.1016/j.bmcl.2006.01.041

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


  2 in total

1.  4-[2-(4-Fluoro-phen-yl)-1H-pyrrol-3-yl]pyridine.

Authors:  Bassam Abu Thaher; Pierre Koch; Dieter Schollmeyer; Stefan Laufer
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-02-04

2.  Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites.

Authors:  Alexios N Matralis; Adnan Malik; Maria Penzo; Inmaculada Moreno; Maria J Almela; Isabel Camino; Benigno Crespo; Anas Saadeddin; Sonja Ghidelli-Disse; Lourdes Rueda; Felix Calderon; Simon A Osborne; Gerard Drewes; Markus Böesche; Elena Fernández-Álvaro; Jose Ignacio Martin Hernando; David A Baker
Journal:  J Med Chem       Date:  2019-10-14       Impact factor: 7.446

  2 in total

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