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一些1-(2,4-二羟基硫代苯甲酰基)咪唑、咪唑啉和四唑的合成及其对念珠菌属的强效活性。

Synthesis of some 1-(2,4-dihydroxythiobenzoyl)imidazoles, -imidazolines and -tetrazoles and their potent activity against Candida species.

作者信息

Matysiak Joanna, Niewiadomy Andrzej, Krajewska-Kułak Elzbieta, Macik-Niewiadomy Grazyna

机构信息

Department of Chemistry, University of Agriculture, Akademicka 15, 20-950 Lublin, Poland.

出版信息

Farmaco. 2003 Jun;58(6):455-61. doi: 10.1016/S0014-827X(03)00046-6.

Abstract

Various 1-(2,4-dihydroxythiobenzoyl)imidazoles, -imidazolines and -tetrazoles were synthesized and evaluated for their in vitro antifungal activity. Compounds were prepared by the reaction of sulfinyl-bis-(2,4-dihydroxythiobenzoyl) with properly substituted azoles. The MIC values against the Candida albicans ATCC 10231 strain, the azole-resistant clinical isolates of C. albicans and non-Candida species were determined. Tetrazole derivatives were the most active against C. albicans, imidazoline derivatives against non-Candida species. All compounds showed higher activity than that of comparable drugs.

摘要

合成了多种1-(2,4-二羟基硫代苯甲酰基)咪唑、咪唑啉和四唑,并对其体外抗真菌活性进行了评估。通过亚磺酰基-双-(2,4-二羟基硫代苯甲酰基)与适当取代的唑类反应制备化合物。测定了对白色念珠菌ATCC 10231菌株、白色念珠菌唑类耐药临床分离株和非念珠菌属的最低抑菌浓度(MIC)值。四唑衍生物对白色念珠菌活性最强,咪唑啉衍生物对非念珠菌属活性最强。所有化合物均表现出比同类药物更高的活性。

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