1,2,3,4-四氢-4-氧代-1,8-萘啶-3-羧酸酯、腈和羧酰胺的合成及抗菌活性评价
Synthesis and antibacterial evaluation of 1,2,3,4-tetrahydro-4-oxo-1,8-naphthyridine-3-carboxylic acid esters, carbonitriles, and carboxamides.
作者信息
Santilli A A, Scotese A C, Yurchenco J A
出版信息
J Med Chem. 1975 Oct;18(10):1038-41. doi: 10.1021/jm00244a021.
A series of 1,2,3,4-tetrahydro-4-oxo-1,8-naphthyridine-3-carboxylic acid esters, carbonitriles, and carboxamides (2a-k) was synthesized and initially evaluated (dose range 50-400 mg/kg) in mice infected with Escherichia coli. Only two derivatives, the ethyl and butyl esters of 1-ethyl-1,2-dihydro-4-hydroxy-7-methyl-1,8-naphthyridine-3-carboxylic acid, protected the animals against E. coli and several other gram-negative bacterial pathogenic infections. A pro-drug type of mechanism appears to be operable since neither agent showed in vitro activity.
合成了一系列1,2,3,4-四氢-4-氧代-1,8-萘啶-3-羧酸酯、腈和羧酰胺（2a - k），并在感染大肠杆菌的小鼠中进行了初步评估（剂量范围为50 - 400 mg/kg）。只有两种衍生物，即1-乙基-1,2-二氢-4-羟基-7-甲基-1,8-萘啶-3-羧酸的乙酯和丁酯，能保护动物免受大肠杆菌和其他几种革兰氏阴性细菌病原体感染。由于这两种药物在体外均无活性，因此似乎存在前药型作用机制。
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