Synthesis and SAR of 2, 3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents

…, R Bugianesi, J Simeone, L Chang, A Gurnett…

Index: Biftu, Tesfaye; Feng, Dennis; Ponpipom, Mitree; Girotra, Narindar; Liang, Gui-Bai; Qian, Xiaoxia; Bugianesi, Robert; Simeone, Joseph; Chang, Linda; Gurnett, Anne; Liberator, Paul; Dulski, Paula; Leavitt, Penny Sue; Crumley, Tami; Misura, Andrew; Murphy, Terence; Rattray, Sandra; Samaras, Samantha; Tamas, Tamas; Mathew, John; Brown, Christine; Thompson, Don; Schmatz, Dennis; Fisher, Michael; Wyvratt, Matthew Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 13 p. 3296 - 3301

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Citation Number: 29

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 ...