Title of article :
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
Author/Authors :
Tesfaye Biftu، نويسنده , , Dennis Feng، نويسنده , , Mitree Ponpipom، نويسنده , , Narindar Girotra، نويسنده , , Gui-Bai Liang، نويسنده , , Xiaoxia Qian، نويسنده , , Robert Bugianesi، نويسنده , , Joseph Simeone، نويسنده , , Linda Chang، نويسنده , , Anne Gurnett، نويسنده , , Paul Liberator، نويسنده , , Paula Dulski، نويسنده , , Penny Sue Leavitt، نويسنده , , Tami Crumley، نويسنده , , Andrew Misura، نويسنده , , Terence Murphy، نويسنده , , Sandra Rattray، نويسنده , , Samantha Samaras، نويسنده , , Tamas Tamas، نويسنده , , John Mathew، نويسنده , , et al.، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
Pages :
6
From page :
3296
To page :
3301
Abstract :
Several analogs of 2,3-diaryl pyrroles were synthesized and evaluated as inhibitors of Eimeria tenella cGMP-dependent protein kinase and in in vivo anticoccidial assays. A 4-fluorophenyl group enhances both in vitro and in vivo activities. The most potent analogs are the 5-(N-methyl, N-ethyl, and N-methylazetidine methyl) piperidyl derivatives 12, 23, and 34. These compounds have a broad spectrum of activity. Based on the in vivo efficacy and cost of synthesis, the N-ethyl analog 23 was chosen as a novel anticoccidial agent for a field trial.
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2005
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
795776
Link To Document :
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