6-氮杂尿嘧啶的抗球虫衍生物。3. 含磺酰胺取代基的1-苯基-6-氮杂尿嘧啶的合成、高活性及短血浆半衰期
Anticoccidial derivatives of 6-azauracil. 3. Synthesis, high activity, and short plasma half-life of 1-phenyl-6-azauracils containing sulfonamide substituents.
作者信息
Miller M W, Mylari B L, Howes H L, Figdor S K, Lynch M J, Lynch J E, Koch R C
出版信息
J Med Chem. 1980 Oct;23(10):1083-7. doi: 10.1021/jm00184a005.
PMID:6893468
Abstract
A series of 1-phenyl-6-azauracils containing sulfonamide substituents was prepared. In contrast to previous 1-phenyl-6-azauracils, some of these sulfonamides combine high activity against Eimeria tenella infections in chickens with a very rapid rate of clearance from plasma. Most active was 1-[3'-chloro-5'-methyl-4'-(morpholinylsulfonyl)phenyl]-6-azauracil, with a minimum effective concentration in feed of about 10 ppm.
摘要
制备了一系列含有磺酰胺取代基的1-苯基-6-氮杂尿嘧啶。与先前的1-苯基-6-氮杂尿嘧啶不同，其中一些磺酰胺对鸡的柔嫩艾美耳球虫感染具有高活性，且从血浆中清除的速度非常快。活性最高的是1-[3'-氯-5'-甲基-4'-(吗啉基磺酰基)苯基]-6-氮杂尿嘧啶，饲料中的最低有效浓度约为10 ppm。
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