A Novel Synthesis of the Efficient Anti-Coccidial Drug Halofuginone Hydrobromide
AbstractBackground: Halofuginone hydrobromide (1) is recognized as an effective drug against several species of Eimeria (E.) in poultry. In this paper, we describe a convenient and low cost preparation method for the compound, as well as primary validation of its activity. Methods: First, 7-bromo-6-chloroquinazolin-4(3H)-one (2) was prepared from m-chlorotoluene by a conventional process, and then chloroacetone was creatively introduced in two steps. Finally, halofuginone hydrobromide (1) was obtained from 7-bromo-6-chloro-3-(3-cholroacetonyl) quinazolin-4(3H)-one (4) by a four-step reaction sequence including condensation, cyclization, deprotection and isomerization. The structures of the relative intermediates and target compound were characterized by melting point, IR, MS and 1H-NMR. Besides, the protective effect of compound 1-supplemented chicken diet at doses of 6, 3 and 1.5 mg per 1 kg were evaluated on chickens infected with E. tenella, by reduction in mortality, weight loss, fecal oocyst excretion and gut pathology, respectively. Results: Halofuginone hydrobromide (1) was prepared successfully by and improved and innovative method based on traditional research. Moreover, the synthesized halofuginone hydrobromide significantly exhibited an anti-coccidial property. Conclusions: The fruitful work described in this Communication has resulted in halofuginone hydrobromide, which has a good pharmaceutical development prospects, becoming more available for large-scale production. View Full-Text
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Zhang, J.; Yao, Q.; Liu, Z. A Novel Synthesis of the Efficient Anti-Coccidial Drug Halofuginone Hydrobromide. Molecules 2017, 22, 1086.
Zhang J, Yao Q, Liu Z. A Novel Synthesis of the Efficient Anti-Coccidial Drug Halofuginone Hydrobromide. Molecules. 2017; 22(7):1086.Chicago/Turabian Style
Zhang, Junren; Yao, Qizheng; Liu, Zuliang. 2017. "A Novel Synthesis of the Efficient Anti-Coccidial Drug Halofuginone Hydrobromide." Molecules 22, no. 7: 1086.
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