Isolation, structure, and coccidiostat activity of coccidiostatin A.
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.
Jayasuriya
Hiranthi
H
Merck Research Laboratories, P. O. Box 2000, Rahway, New Jersey 07065, USA. hiranthi_jayasuriya@merck.com
Guan
Ziqiang
Z
Dombrowski
Anne W
AW
Bills
Gerald F
GF
Polishook
Jon D
JD
Jenkins
Rosalind G
RG
Koch
Leslie
L
Crumley
Tami
T
Tamas
Tamas
T
Dubois
Michelle
M
Misura
Andrew
A
Darkin-Rattray
Sandra J
SJ
Gregory
Lynn
L
Singh
Sheo B
SB
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*
D003049:Coccidiostats; D006572:Heterocyclic Compounds, Bridged-Ring; C523227:coccidiostatin A