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异喹啉衍生物的研究。IV. N2-亚芳基取代的3-咔唑基异喹啉的抗菌和抗真菌活性的合成与评价。

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

作者信息

Vittorio F, Pappalardo M S, Ronsisvalle G, Blandino G

机构信息

Istituto di Chimica Farmaceutica e Tossicologica, Universita' di Catania, Italy.

出版信息

Farmaco Sci. 1988 Mar;43(3):239-50.

PMID:3417009
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.

摘要

已合成了2,4-二甲基-1-氧代-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,并对其进行了体外抗菌和抗真菌活性测试。1-(1-氯-4-甲基-3-异喹啉甲酰基)-2-(5-硝基-2-糠叉基)肼(VII h)在该系列中被证明是最有效的(最低抑菌浓度为0.78微克/毫升),并且对几种金黄色葡萄球菌菌株的效力比呋喃唑酮更强;该化合物还表现出中等程度的抗真菌活性。

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