1-乙基-6-氟-1,4-二氢-4-氧-7-(哌嗪-1-基)-3-喹诺线羧酸(诺氟沙星)衍生物的合成。

Il Farmaco; edizione scientifica Pub Date : 1988-06-01
M Pappalardo, A Omodei-Salè, G Zanuso, A Gutierrez, L Moujir, F G De Las Heras
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引用次数: 0

摘要

为了研究哌嗪环上仲氮取代基对抗菌活性的影响,合成了12种与诺氟沙星结构相近的新型氟喹诺酮类药物。在多种革兰氏阳性和革兰氏阴性生物上测试的新物质(氨基甲酸酯、异脲类、胍类、脲类和氰胺类)的活性低于模型化合物。
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Synthesis of some derivatives of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(piperazin-1-yl)-3-quino linecarbo xylic acid (norfloxacin) as potential antibacterial agents.

Twelve new fluoroquinolones, structurally related to norfloxacin, have been synthesized in order to investigate the effect of substituents at the secondary nitrogen of the piperazine ring on antimicrobial activity. The new substances (carbamates, isoureas, guanidines, ureas and cyanamides) tested on a variety of gram-positive and gram-negative organisms showed lower activity than the model compound.

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Synthesis, binding affinities for alpha-adrenoceptor and eudismic analysis of chiral benzodioxane derivatives and their chiral opened analogues. Prolyl derivatives of enalapril as potential angiotensin converting enzyme inhibitors. Synthesis, structure and activity of a few open models related to classic H2-antagonists. Benzodioxanes and quinazolines: probes for characterizing alpha-adrenoreceptors. Isolation and structure determination of the main related substances of teicoplanin, a glycopeptide antibiotic.
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