| Literature DB >> 15922595 |
Tesfaye Biftu1, Dennis Feng, Mitree Ponpipom, Narindar Girotra, Gui-Bai Liang, Xiaoxia Qian, Robert Bugianesi, Joseph Simeone, Linda Chang, Anne Gurnett, Paul Liberator, Paula Dulski, Penny Sue Leavitt, Tami Crumley, Andrew Misura, Terence Murphy, Sandra Rattray, Samantha Samaras, Tamas Tamas, John Mathew, Christine Brown, Don Thompson, Dennis Schmatz, Michael Fisher, Matthew Wyvratt.
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.Entities:
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Year: 2005 PMID： 15922595 DOI： 10.1016/j.bmcl.2005.04.060
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823