title: Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.
abstract: Parasite cGMP-dependent protein kinase (PKG) has been recently validated as a biochemical target for the treatment of coccidiosis. To discover new anticoccidial leads, we have screened our library of natural product extracts for inhibitors of parasite PKG. Bioassay-guided fractionation of the microbial extracts has led to the discovery of tenellones A (2) and B (3), two new highly substituted benzophenones. The isolation, structure, and activity of these compounds are described.
authors.affiliation: Natural Products Chemistry and Human and Animal Infectious Disease, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
authors.forename: Chaowei
authors.initials: C
authors.lastname: Zhang
authors.forename: John G
authors.initials: JG
authors.lastname: Ondeyka
authors.forename: Kithsiri B
authors.initials: KB
authors.lastname: Herath
authors.forename: Ziqiang
authors.initials: Z
authors.lastname: Guan
authors.forename: Javier
authors.initials: J
authors.lastname: Collado
authors.forename: Gonzalo
authors.initials: G
authors.lastname: Platas
authors.forename: Fernando
authors.initials: F
authors.lastname: Pelaez
authors.forename: Penny S
authors.initials: PS
authors.lastname: Leavitt
authors.forename: Anne
authors.initials: A
authors.lastname: Gurnett
authors.forename: Bakela
authors.initials: B
authors.lastname: Nare
authors.forename: Paul
authors.initials: P
authors.lastname: Liberator
authors.forename: Sheo B
authors.initials: SB
authors.lastname: Singh
mesh_terms: D000818:Animals; D001577:Benzophenones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D017869:Cyclic GMP-Dependent Protein Kinases; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D005658:Fungi / Q000737:chemistry*; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry; D013030:Spain; D014122:Toxoplasma / Q000378:metabolism
chemical_list: D001577:Benzophenones; D004791:Enzyme Inhibitors; C501148:tenellone A; C501149:tenellone B; D017869:Cyclic GMP-Dependent Protein Kinases