Abstract:
:During the course of a collaborative screening program, a set of 1-phenyl-4-pyridyl-butadienes was found to exhibit in vitro activity against Eimeria tenella in a cell-based assay. Activity was dependent on the chain length and degree of unsaturation of the linker between the two aryl groups as well as substitution of the pyridine moiety. Structure-activity relationship studies were subsequently conducted over a larger range of 1,4-diarylbutadienes in order to determine the scope of active compounds, to identify structural patterns governing activity and to enhance in vitro potency against E. tenella. In addition, the efficacy of many compounds for treating coccidiosis in chickens was measured by testing the ability of the compound to prevent or reduce intestinal and cecal lesions when administered by oral gavage. A few compounds in the series were identified that exhibited a moderate degree of in vitro and in vivo activity.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Gage JL,Kirst HA,O'Neil D,David BA,Smith CK 2nd,Naylor SAdoi
10.1016/s0968-0896(03)00330-4subject
Has Abstractpub_date
2003-09-01 00:00:00pages
4083-91issue
18eissn
0968-0896issn
1464-3391pii
S0968089603003304journal_volume
11pub_type
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