Highly Substituted Terphenyls as Inhibitors of Parasite cGMP-Dependent Protein Kinase Activity

Parasite cGMP-dependent protein kinase (PKG) is one of the validated biochemical targets for the treatment of coccidiosis. We screened our library of natural product extracts for inhibitors of parasite PKG for the discovery of anticoccidial leads. Terferol (1) and three new terphenyls (2, 3, and 4)...

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Veröffentlicht in:	Journal of natural products (Washington, D.C.) D.C.), 2006-04, Vol.69 (4), p.710-712
Hauptverfasser:	Zhang, Chaowei, Ondeyka, John G, Herath, Kithsiri B, Guan, Ziqiang, Collado, Javier, Pelaez, Fernando, Leavitt, Penny S, Gurnett, Anne, Nare, Bakela, Liberator, Paul, Singh, Sheo B
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics (antibacterial agents, antifungal agents) Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents Applied microbiology Ascomycota - chemistry Biological and medical sciences Coccidiosis - drug therapy Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors Eimeria tenella - drug effects Enzyme Inhibitors - chemistry Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - pharmacology France Fundamental and applied biological sciences. Psychology Microbiology Molecular Structure Terphenyl Compounds - chemistry Terphenyl Compounds - isolation & purification Terphenyl Compounds - pharmacology
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Zusammenfassung:	Parasite cGMP-dependent protein kinase (PKG) is one of the validated biochemical targets for the treatment of coccidiosis. We screened our library of natural product extracts for inhibitors of parasite PKG for the discovery of anticoccidial leads. Terferol (1) and three new terphenyls (2, 3, and 4) were isolated using bioassay-guided fractionation of the microbial extract of a Phoma sp. by a high-throughput two-step isolation method employing LH-20 and reversed-phase HPLC. These compounds inhibited parasite PKG with IC50 values in the range 0.9−5.8 μM.
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np0505418