Synthesis and antibacterial activities of substituted 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyl ic acids.
Synthesis and antibacterial activities of substituted 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyl ic acids.
复制标题
取代的7-氧代-2,3-二氢-7H-吡啶并[1,2,3-de][1,4]苯并恶嗪-6-羧酸的合成和抗菌活性。
DOI：
10.1248/cpb.32.4907
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发表时间：
1984
影响因子：
1.7
通讯作者：
Yoshiaki Tanaka
中科院分区：
文献类型：
--
作者：
I. Hayakawa;T. Hiramitsu;Yoshiaki Tanaka
作为寻找新的合成抗菌剂以对抗全身感染的一部分，合成了7-氧代-2，3-二氢-7H-吡啶并[1，2，3-de][1，4]苯并恶嗪-6-羧酸的各种类似物。在新合成的化合物中，9-氟-3-甲基-10-（4-甲基-1-哌嗪基）-7-氧代-2，3-二氢-7H-吡啶并[1，2，3-de][1，4]苯并恶嗪-6-羧酸（DL-8280）对革兰氏阳性和阴性病原体（包括铜绿假单胞菌）显示出有效的抗菌活性，并且在单独的实验中显示其代谢处置是有利的。
As part of a search for new synthetic antibacterial agents to combat systemic infection, various analogues of 7-oxo-2, 3-dihydro-7H-pyrido [1, 2, 3-de] [1, 4] benzoxazine-6-carboxylic acids were synthesized. Among the compounds newly synthesized, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2, 3-dihydro-7H-pyrido [1, 2, 3-de] [1, 4] benzoxazine-6-carboxylic acid (DL-8280) showed potent antibacterial activity against Gram-positive and-negative pathogens, including Psedomonas aeruginosa, and its metabolic disposition was shown in separate experimentals to be favorable.