Coccidiostatic activity

Various other properties intestinal antiseptic (932, 933), fungicide (934, 935), insecticide (895. 898), coccidiostatic activity (936), car-cinolytic activity (937), radioprotective activity (938), antimutagenic activity (939, 940). 

The discovery of the coccidiostat activity of monensin marks the second milestone in the history of the use of fermentation products in agriculture. Until this discovery, the emphasis had been on the search for antibiotics with antibacterial activity. It was now evident that fermentation products could be used for the control of parasitic infections. 

It is administered continuously with the feed at a dose of 200 ppm for rabbits and 125 ppm for chickens. A mixture with methylbenzoquate is also available for prevention of coccidiosis in chickens and turkeys. Clopidol is more coccidiostatic than coccidiocidal. Its coccidiostatic activity may hold tire sporozoite undeveloped in the host cell for as long as 60 days if the drug is withdrawn during this static phase, latent coccidiosis may appear as the parasite resumes development. For clopidol, a withdrawal period of 5 days has been set for all animal species. 

The search for medicinal applications of crown ethers and cryptands has so far led to only a few pre-clinical studies. Many of the crown ethers and natural ionophores are toxic. Presumably the toxicity arises from the slow leakage of potassium out of cells and of sodium into cells. Antibacterial activity has been noted for several crown ethers and found to parallel potassium transport276). The established coccidiostatic activity of ionophores has led to the screening of crown ethers for coccidiostatic activity277). As yet the synthetic ionophores have shown no evidence of superiority over their natural product counterparts. 

Many examples of a variety of alkyl 4-hydroxy-6,7-dialkoxy-quinoline-3-carboxylates (X) were found to possess a high order of coccidiostatic activity when tested for prevention of experimental Eimeria tenella infections in chicks.xhe preferred examples were... 

Budesinsky et al. (209) have prepared a number of 3-(3-amino-2-hydroxypro-pyl)- and 3-(3-aminoacetonyl)-quinazolin-4-ones in which the 3-piperidinol part of febrifugine has been replaced by readily available bases (aniline, pyrrolidine, etc.). These compounds show a decrease in coccidiostatic activity and marked activity against Eimeria tenella, Nippostrongylus brasiliensis, and Fasciola hepatica. 

The triazinedione, triazuril (163) is active as a poultry coccidiostat. Diazonium salt 160, prepared from the appropriate aniline, is coupled with the active methylene group of N-carbethoxycyanoacetamide to give 161. Hydrolysis of the cyano group is accompanied by cyclization, and the resulting acid (162) is decarboxylated to triazuril (163) on heating.50... 

Some of the N-alkylated narceine amides and imides were tested for antibacterial effectiveness and showed activity of medium potency against Mycobacterium tuberculosis H37 Rv. Their antimycotic activity was also of medium strength. Coccidiostatic screening showed some effectiveness (100). 

Monensin has been shown to form within the body more than 50 metabolites, among which the glucoside metabolite is also active as a coccidiostat (26). Clear evidence of the extensive monensin metabolism has been provided by another study based on the administration of radiolabeled monensin to chickens... 

There are no effective agents in use at present but the coccidiostat, halofuginone (67), is active in laboratory tests against T. parva and T. annulata. 

Sulfanilamides, 1, 145 carbonic anhydrase inhibition by, 1, 173 Sulfaphenazole antibacterial activity, 5, 291 Sulfapyridine, 1, 161 as antibacterial, 2, 517 veterinary use, 1, 209 Sulfaquinoxaline coccidiostat veterinary use, 1, 212 Sulfasomidine, 3, 151 Sulfasomizole... 

Amino-3- 3,4-dichlorobenzyl)-1,2,3-triazole-5-carboxamide, and related compounds, made by condensing an azide with cyanoacetamide, were strongly coccidiostatic, even at a dilution of 0.001%, in chicken feed (85EUP151528). Several 3-[4-(4-chlorobenzoyl)benzyl analogs had similar activity (85EUP151529). 

The main search for biologically active quinoxalines has centered around the preparation of quinoxaline iV-oxides. 3-Substituted 2-methylquinoxaline 1,4-dioxides with high antibacterial activity have been prepared (Chapter IV). Quinoxaline 2-sulfonamide has had sustained use as a coccidiostat for poultry (Chapter XI). A series of naturally occurring quinoxaline antibiotics, the quinomycins and triostins, are known, but their therapeutic index is low (Chapter IX). 

TABLE 2.16 Sales of Therapeutic AMDs and Coccidiostats in UK in 2003 and 2008 (Metric Tons of Active Ingredient)... 

Mr 724.97, mp. 183.5-185 °C. A polyether antibiotic from cultures of Streptomyces hygro-scopicus and other streptomycetes. N. acts as an ion-ophore for monovalent cations in mitochondria, is active against Gram-positive bacteria and is used as a coccidiostatic agent... 

Febrifugine is also a powerful emetic (with a low therapeutic index) and is one of the most effective coccidiostatics known. 6-Chloro-7-bromofebrifugine is active prophylactically against Eimeria tenella when added to fodder at a level of0.0003% 217,227). Bude insky et al. 28) have... 

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