STRUCTURAL MODIFICATION OF FEBRIFUGINE - SOME METHYLENEDIOXY ANALOGS
STRUCTURAL MODIFICATION OF FEBRIFUGINE - SOME METHYLENEDIOXY ANALOGS
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DOI：
10.1021/jm00299a018
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发表时间：
1970-01-01
影响因子：
7.3
通讯作者：
CHENG, CC
中科院分区：
文献类型：
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作者：
CHIEN, PL;CHENG, CC
与常量 (I) 相关的催吐特性 2-4 限制了其作为抗疟疾化疗药物的潜在用途。 5 对该化合物进行适当的结构修饰可以减少其不良毒性作用。已经描述了本系列中的一些综合工作。 6-9 常健的侧链修饰尚未发现富有成效；另一方面，喹唑啉环系统上的某些基团，特别是在位置5、6和7处的6-10的单取代或二取代，导致抗疟活性增加，并且在某些情况下，还增加了化疗指数。
The emetic property2-4 associated with febrifugine (I) has limited its potential usefulness as a chemotherapeutic agent against malaria. 5 Suitable structural modification of this compound may reduce its unde-sired toxic effect. Some synthetic work in this series has been described. 6-9 Side-chain modification of febrifugine had not been found fruitful; 6-10 on the other hand, mono- or disubstitution by certain groups on the quinazoline ring system, particularly at positions 5, 6, and 7, resulted in increased antimalarial activity and, in some cases, also increased the chemotherapeutic index.