取代的咪唑并[2,3-α]吡啶-2-氨基甲酸酯驱虫药。
Substituted imidazo[2,3-alpha]pyridine-2-carbamate anthelmintics.
作者信息
Bochis R J, Olen L E, Waksmunski F S, Mrozik H, Eskola P, Kulsa P, Wilks G, Taylor J E, Egerton J R, Ostlind D A, Olson G
出版信息
J Med Chem. 1981 Dec;24(12):1518-21. doi: 10.1021/jm00144a030.
Anthelmintic efficacies of a series of 6-substituted methyl imidazo[1,2-alpha]pyridine-2-carbamates were compared to similarly substituted benzimidazole-2-carbamates. With only one exception, methyl 6-benzoylimidazo[1,2-alpha]pyridine-2-carbamate, both classes of compounds exhibited similar activity vs. Nematospiroides dubius in mice. Preliminary screening indicated methyl 6-(1,2,2-trichloroethenyl)imidazo[1,2-alpha]pyridine-2-carbamate to be the most potent derivative in the series. However, evaluation in sheep indicated that its anthelmintic spectrum was inferior to methyl 6-(phenylsulfinyl)imidazo[1,2-alpha]pyridine-2-carbamate.
将一系列6-取代甲基咪唑并[1,2-α]吡啶-2-氨基甲酸酯的驱虫效果与类似取代的苯并咪唑-2-氨基甲酸酯进行了比较。除了一个例外，即6-苯甲酰基咪唑并[1,2-α]吡啶-2-氨基甲酸甲酯，这两类化合物对小鼠体内的双盲肠线虫均表现出相似的活性。初步筛选表明，6-(1,2,2-三氯乙烯基)咪唑并[1,2-α]吡啶-2-氨基甲酸甲酯是该系列中最有效的衍生物。然而，在绵羊身上的评估表明，其驱虫谱不如6-(苯基亚磺酰基)咪唑并[1,2-α]吡啶-2-氨基甲酸甲酯。
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