8-羟基喹啉类似物作为牙菌斑抑制剂的合成及体外评价
Synthesis and in vitro evaluation of 8-hydroxyquinoline analogs as inhibitors of dental plaque.
作者信息
Warner V D, Sane J N, Mirth D B, Turesky S S, Soloway B
出版信息
J Med Chem. 1976 Jan;19(1):167-9. doi: 10.1021/jm00223a031.
PMID:812992
Abstract
A group of 5-substituted 8-hydroxyquinolines with predicted log P values in the 1-4 range has been prepared from either 8-hydroxyquinoline or its appropriate derivative. 5-Formyl-, 5-iodo-, 5-fluoro-, 5-acetyl-, and 5-methoxymethyl-8-hydroxyquinoline in addition to methyl-5(8-hydroxyquinolyl)acetate and ethyl 5-(8-hydroxyquinolyl)acetate displayed greater in vitro antiplaque activity than 8-hydroxyquinoline.
摘要
已从8-羟基喹啉或其合适的衍生物制备出一组预测log P值在1-4范围内的5-取代8-羟基喹啉。除了5-(8-羟基喹啉基)乙酸甲酯和5-(8-羟基喹啉基)乙酸乙酯外，5-甲酰基-、5-碘-、5-氟-、5-乙酰基-和5-甲氧基甲基-8-羟基喹啉在体外显示出比8-羟基喹啉更强的抗牙菌斑活性。
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