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新型1,3-苯并恶唑-2(3H)-酮衍生物系列的合成及生物活性

Synthesis and biological activity of novel series of 1,3-benzoxazol-2(3H)-one derivatives.

作者信息

Krawiecka Mariola, Kuran Bozena, Kossakowski Jerzy, Kierzkowska Marta, Młynarczyk Grazyna, Cieślak Marcin, Kaźmierczak-Barańska Julia, Królewska Karolina, Dobrowolski Michał A

机构信息

Department of Medical Chemistry, Medical University of Warsaw, 3 Oczki St., 02-007 Warszawa, Poland.

出版信息

Acta Pol Pharm. 2013 Mar-Apr;70(2):245-53.

Abstract

In the search for novel biological agents, a series of new derivatives N-substituted 1,3-benzoxazol-2(3H)-one, 5-chloro-1,3-benzoxazol-2(3H)-one, 6-bromo-1,3-benzoxazol-2(3H)-one were prepared. All of the compounds were characterized by 1H NMR, 13C NMR and ESI MS spectra. Moreover, for compound 1 an Xray structure was determined. All derivatives were tested for antimicrobial activity against a selection of Gram-positive, Gram-negative bacteria and yeasts. The selected compounds (2-8, 10) were tested for their cytotoxic properties in K562, HeLa and normal cells.

摘要

在寻找新型生物制剂的过程中,制备了一系列新的衍生物N-取代的1,3-苯并恶唑-2(3H)-酮、5-氯-1,3-苯并恶唑-2(3H)-酮、6-溴-1,3-苯并恶唑-2(3H)-酮。所有化合物均通过1H NMR、13C NMR和ESI MS光谱进行了表征。此外,还测定了化合物1的X射线结构。对所有衍生物针对一系列革兰氏阳性菌、革兰氏阴性菌和酵母菌进行了抗菌活性测试。对所选化合物(2-8、10)在K562、HeLa细胞和正常细胞中进行了细胞毒性特性测试。

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