STRUCTURE AND ANTICOCCIDIAL ACTIVITY AMONG SOME 4-HYDROXYQUINOLINECARBOXYLATES
STRUCTURE AND ANTICOCCIDIAL ACTIVITY AMONG SOME 4-HYDROXYQUINOLINECARBOXYLATES
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DOI：
10.1021/jm00299a019
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发表时间：
1970-01-01
影响因子：
7.3
通讯作者：
STEVENS, GD
中科院分区：
文献类型：
--
作者：
MIZZONI, RH;GOBLE, F;STEVENS, GD
(4)第6位和第7位的替换似乎对更好的活动是必不可少的。我们对这类化合物的长期兴趣源于与另一个问题的联系。在另一个系列中开发的铅的应用得到了活性环丙氨酸乙酯6.7-双(环丙基甲氧基)-4-羟基-3<；异丙酚羧酸乙酯。3这种底物的高生物活性促使了对4-7类化合物的全面研究。4和5的制备方法如方案I所示。由r/j-乙酰氧基乙酰苯胺(方案II)制备6类化合物，7通过将相同的合成序列应用于对酰氧基苯乙胺而得到。
(4) Substitution in the 6 and 7 positions seems to be essential for superior activity. Our longtime interest in this class of compounds originated in connectionwith another problem. Applications of a lead developed in another series gave ethyl 6.7-bis (cyclopropylmethoxy)-4-hydroxy-3-< iuinolinecarboxylate (cyproquinidate), an active coc-cidiostat. 3 The high biological activity of this sub-stance prompted a comprehensive study In include compounds of types 4-7.The preparation of 4 and 5 was carried out in a con-ventional manner as shown in Scheme I. Compounds of type 6 were prepared from r/j-acvloxyacetanilide (Scheme II) and 7 resulted by application of the same synthetic sequence to the p-acyloxyncet-, anilide.