Toltrazuril

Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites.Target: AntiparasiticToltrazuril is an antiprotozoal agent that acts upon Coccidia parasites. Toltrazuril induces changes in the fine structure of coccidian development stages that are mainly due to a swelling of the endoplasmatic reticulum and of the Golgi apparatus and to abnormalities in the peri-nuclear space, disturbance in nuclear division. Treated with toltrazuril showed a considerably lower mean opg to that o

Toltrazuril (Baycox®,Procox®) is a triazinon drug thathas broad-spectrum anticoccidial and antiprotozoalactivity. It is not commercially available in the UnitedStates, but it is available in other countries. It is activeagainst both asexual and sexual stages of coccidia byinhibiting nuclear division of schizonts and microga-monts and the wall-forming bodies of macrogamonts. Itmay also be useful in the treatment of neonatal porcinecoccidiosis, EPM, and canine hepatozoonosis.Toltrazuril and its major metabolite ponazuril (toltrazuril sulfone, Marquis) are triazine-based antiprotozoal drugs that have specific activity against apicomplexan coccidial infections. Toltrazuril is not available within the United States.

ChEBI: 1-methyl-3-[3-methyl-4-[4-(trifluoromethylthio)phenoxy]phenyl]-1,3,5-triazinane-2,4,6-trione is an aromatic ether.

1)Weigh 50 g of tolazuril into a 2000 mL three-necked flask, add 600 mL of acetone, Stirring at room temperature to obtain a white turbid emulsion; 2) weighed 8. 39g potassium hydroxide placed in the beaker, then add acetone, stirring until the complete dissolution of sodium hydroxide, the preparation of Into a mass percentage concentration of 6% sodium hydroxide acetone solution; 3) A solution of sodium hydroxide in acetone in step 2) was added dropwise at a rate of 1 mL / min to the emulsion in step 1) After the completion of the dropwise addition, the solution was gradually clarified, and the reaction was continued for 3 hours. After TLC indicated that the starting material had been reacted, the reaction solution was dried to give a viscous white solid, followed by addition of sufficient methanol to dehydrate, The water was removed to give 43. 13 g of crude tolazolinate in white, with a yield of 73.9%. 4) Ethanol and ethyl acetate were mixed in a volume ratio of 13: 3 as a mixed organic solvent, And the mixture was stirred for 6 hours. After the solution was separated into layers, the reaction solution was suction-filtered and the filter cake was dried for 12 hours. Then, To give 36. 7 g of the white salt of tolzetil. The substance was detected by TLC and did not contain tolazuril. MS: m / z = 424, NMR: [1 H] NMR: TMS as internal standard, deuterated DMS0 as solvent, delta7.73-7.71 (2 Eta, Mu); delta (2H, m); delta 3.08 (3Hz, s); delta 2.12 (3H, s). From the above analysis, it was found that the white solid was {1- [3-methyl-4 (4-trifluoromethylthio-phenoxy) -phenyl] -3-methyl- 2, 4, 6-triketone} potassium salt, i.e., tolcyclidine potassium salt, which has the following structure:1) weighed 50g Toluconazole into 2000mL three-necked flask, then add 650mL ethanol, stirring at room temperature to get white turbid emulsion; 2) weighed 9. 8g potassium hydroxide in a beaker, then add ethanol, stirring until the complete dissolution of potassium hydroxide, the concentration of the preparation of 7% concentration of potassium hydroxide ethanol solution; 3) The potassium hydroxide ethanol solution in step 2) was added dropwise to the emulsion in step 1) at a rate of 1 mL / min under stirring. After completion of the dropwise addition, stirring was continued for 4 hours, and the solution was gradually clarified After TLC indicated that the starting material had reacted, the reaction solution was dried to give a viscous white solid which was further dehydrated by addition of petroleum ether, dried by dewatering and then dried to obtain 55. 05 g of white Toluconazole potassium salt crude product yield 92.5%, petroleum ether can be used isopropyl alcohol, ethyl acetate or acetone instead. 4)Mix acetone and ethyl acetate in a volume ratio of 13: 1 as a mixed organic solvent. In a 1000 mL three-necked flask, add 350 mL of mixed organic solvent and add 50 g of the crude tolzetal potassium salt and stir for 5 hours. Layer, the solution was again suction-filtered and the filter cake was dried for 12 hours to obtain 49 g of white tolazolide potassium salt. The substance was detected by TLC without tolcyfamide. The results of mass spectroscopy and nuclear magnetic resonance (NMR) , MS: m / z = 424, NMR: [1 H] NMR: TMS internal standard, deuterated DMS0 as solvent, delta 7-73-7.71 (2H, (5 H, M); delta 3. 08 (3H, s); Delta 2.12 (3H, s).

Labelled analog of a triazinetrione anticoccidial. Coccidiostat.

Toltrazuril is an antiprotozoal agent that is widely used to prevent coccidia parasite infection in veterinary applications. The effectiveness of treatment appears to depend on the coccidian species, development stage of the parasite, and level of infection.

Labelled analog of a triazinetrione anticoccidial. Coccidiostat. Toltrazuril is found to be highly effective against coccidia and is used in controlling coccidiosis. It is acting against all intracellular development stages of coccidia of the merogony (asexual multiplication) and gamogony (sexual phase). All stages are destroyed, thus the mode of action is coccidiocidal.