McManus, E. C. published the artcileUse of coccidia to study the structure-activity relations of a series of p-aminobenzoic acid antagonists, Computed Properties of 5204-46-6, the publication is Develop. Ind. Microbiol. (1965), 44-7, database is CAplus.
Young coccidiosis-susceptible chicks were fed a standard laboratory ration with graded concentrations of test chemicals added just prior to use. On the 2nd day of the test, the chicks were inoculated orally with 100,000 sporulated oocysts of Eimeria maxima; 6 days later birds were killed and weighed, the small intestine homogenized with water, and the oocysts counted. The min. effective diet concentrations of 28 derivatives of p-aminobenzoic acid (I) were determined together with the percent reduction of oocyst count. Remarkably potent anticoccidial compounds were found in a series of ortho-substituted derivatives of I. Groups with high coccidiostatic activity conferring effects were lower alkoxy, alkylthio, and alkyl amino with approx. similar size and shape. The most active compounds, capable of reducing the oocyst count below 25% were the ο-ethoxy derivative, its esters, and N-acyl derivatives, and the ο-chloro, ο-methoxy, ο-isopropoxy, ο-ethyl, and ο-thioethyl derivatives of I. Me 4-acetamido-2-ethoxybenzoate (ethopabate) (II) reduced the oocyst count to nil. The methyl, chloro, nitro, and methoxy derivatives conferred anticoccidial activity when substituted in the ortho position, but not in meta position. Disubstituted derivatives were inactive. The in vivo anticoccidial activity of II and sulfaquinoxaline (III) was overcome completely by simultaneous administration of I. Both II and III potentiated the anticoccidial activity of pyrimethamine. Cross resistance occurred between II and III for many strains of coccidia. The dose-response curves of II and III were parallel, and their anticoccidial activities were additive. II was about 150-fold more potent than III for control of certain strains of E. maxima and Ε. brunetti, and less potent for Ε. tenella. Both II and III were assumed to inhibit biosynthesis of folic acid-type compounds at different steps in the sequence of reactions for synthesis of tetrahydrofolic acid.
Develop. Ind. Microbiol. published new progress about 5204-46-6. 5204-46-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Amine,Benzene, name is 4-Amino-2,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Computed Properties of 5204-46-6.
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