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位阻邻氨基酚衍生物铜(II)配合物作为抗菌剂的合成与生物学评价

Synthesis and biological evaluation of copper (II) complexes of sterically hindered o-aminophenol derivatives as antimicrobial agents.

作者信息

Loginova Natalia V, Koval'chuk Tat'yana V, Zheldakova Rimma A, Osipovich Nikolai P, Sorokin Victor L, Polozov Genrikh I, Ksendzova Galina A, Glushonok Gennady K, Chernyavskaya Anna A, Shadyro Oleg I

机构信息

Faculty of Chemistry, Belarusian State University, Leningradskaya str. 14, 220050 Minsk, Belarus.

出版信息

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5403-7. doi: 10.1016/j.bmcl.2006.07.065. Epub 2006 Aug 4.

DOI:10.1016/j.bmcl.2006.07.065
PMID:16890430
Abstract

Cu(II) complexes with 4,6-di(tert-butyl)-2-aminophenol (I) and 2-anilino-4,6-di(tert-butyl)phenol (II) have been synthesized and characterized by means of elemental analysis, TG/DTA, FT-IR, UV-vis, ESR, and conductance measurements. The compounds I and II can coordinate in their singly deprotonated forms and behave as bidentate O,N-coordinated ligands; their CuL(2) complexes are characterized by CuN(2)O(2) coordination modes and square planar geometry. In vitro antimicrobial screening against Gram-positive and Gram-negative bacteria, yeasts, and moulds indicated that the compound I and its Cu(II) complex were more active than Questiomycin B, the compound II, and its Cu(II) complex.

摘要

已合成了铜(II)与4,6-二(叔丁基)-2-氨基苯酚(I)和2-苯胺基-4,6-二(叔丁基)苯酚(II)的配合物,并通过元素分析、热重/差示热分析(TG/DTA)、傅里叶变换红外光谱(FT-IR)、紫外可见光谱(UV-vis)、电子顺磁共振(ESR)和电导率测量对其进行了表征。化合物I和II可以以单去质子化形式配位,并表现为双齿O,N配位配体;它们的CuL(2)配合物具有CuN(2)O(2)配位模式和平面正方形几何结构。针对革兰氏阳性菌和革兰氏阴性菌、酵母和霉菌的体外抗菌筛选表明,化合物I及其铜(II)配合物比喹西霉素B、化合物II及其铜(II)配合物更具活性。

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