title: Isolation, structure, and coccidiostat activity of coccidiostatin A.
abstract: Coccidiosis is one of the more common and costly diseases in poultry that is caused by various Eimeria species. In our quest to discover coccidiostats from natural products, we discovered a microbial fermentation extract that exhibited in vivo anticoccidial activity. Fractionation of this extract led to the discovery of two potent antiprotozoals, emecorrugatin A (1) and coccidiostatin A (2). The former compound exhibited only in vitro activity, whereas the latter new compound exhibited in vivo activity against Eimeria species in chickens at 150 ppm dosed in chicken feed. The isolation, structure elucidation, relative configuration, and activity of coccidiostatin A (2) are described.
authors.affiliation: Merck Research Laboratories, P. O. Box 2000, Rahway, New Jersey 07065, USA. hiranthi_jayasuriya@merck.com
authors.forename: Hiranthi
authors.initials: H
authors.lastname: Jayasuriya
authors.forename: Ziqiang
authors.initials: Z
authors.lastname: Guan
authors.forename: Anne W
authors.initials: AW
authors.lastname: Dombrowski
authors.forename: Gerald F
authors.initials: GF
authors.lastname: Bills
authors.forename: Jon D
authors.initials: JD
authors.lastname: Polishook
authors.forename: Rosalind G
authors.initials: RG
authors.lastname: Jenkins
authors.forename: Leslie
authors.initials: L
authors.lastname: Koch
authors.forename: Tami
authors.initials: T
authors.lastname: Crumley
authors.forename: Tamas
authors.initials: T
authors.lastname: Tamas
authors.forename: Michelle
authors.initials: M
authors.lastname: Dubois
authors.forename: Andrew
authors.initials: A
authors.lastname: Misura
authors.forename: Sandra J
authors.initials: SJ
authors.lastname: Darkin-Rattray
authors.forename: Lynn
authors.initials: L
authors.lastname: Gregory
authors.forename: Sheo B
authors.initials: SB
authors.lastname: Singh
mesh_terms: D000818:Animals; D003048:Coccidiosis / Q000209:etiology; D003049:Coccidiostats / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004539:Eimeria / Q000187:drug effects*; D006572:Heterocyclic Compounds, Bridged-Ring / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D015394:Molecular Structure; D010407:Penicillium / Q000737:chemistry*
chemical_list: D003049:Coccidiostats; D006572:Heterocyclic Compounds, Bridged-Ring; C523227:coccidiostatin A