Studies on isoquinoline derivatives. IV. Synthesis and evaluation of the antimicrobial and antifungal activities of N2-arylidene-substituted 3-carbazoyl-isoquinolines.

Il Farmaco; edizione scientifica Pub Date : 1988-03-01
F Vittorio, M S Pappalardo, G Ronsisvalle, G Blandino
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Abstract

2,4-Dimethyl-1-oxo-1,2-dihydro-3-carbazoyl-isoquinoline (II), 1-chloro-, 1-methoxy-3-carbazoyl-4-methylisoquinoline (VI, X) and a series of their hydrazonic derivatives have been synthesized and tested in vitro for antibacterial and antifungal activities. 1-(1-Chloro-4-methyl-3-isoquinolinoyl)-2-(5-nitro-2-furfurylide ne) hydrazine (VII h) proved to be the most effective in the series (MIC 0.78 micrograms/ml) and was more potent than furazolidone against several strains of S.aureus; the same compound also showed a moderate antifungal activity.

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异喹啉衍生物的研究。四、n2 -芳基取代3-咔唑基异喹啉类化合物的合成及抑菌活性评价。
合成了2,4-二甲基-1-氧-1,2-二氢-3-咔唑基异喹啉(II)、1-氯-1-甲氧基-3-咔唑基-4-甲基异喹啉(VI, X)及其一系列腙衍生物,并进行了体外抗菌和抗真菌活性测试。1-(1-氯-4-甲基-3-异喹啉酰基)-2-(5-硝基-2-呋喃烷肼)联氨(VII h)被证明是该系列中最有效的(MIC为0.78微克/毫升),对几种金黄色葡萄球菌的抑制作用强于呋喃唑酮;同样的化合物也显示出适度的抗真菌活性。
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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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