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Synthesis and evaluation of a series of 1,4-diarylbutadienes for anticoccidial activity.

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 Chem

journal_title

Bioorganic & medicinal chemistry

authors

Gage JL,Kirst HA,O'Neil D,David BA,Smith CK 2nd,Naylor SA

doi

10.1016/s0968-0896(03)00330-4

subject

Has Abstract

pub_date

2003-09-01 00:00:00

pages

4083-91

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968089603003304

journal_volume

11

pub_type

杂志文章

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