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Pt(II) and Ag(I) complexes with acesulfame: Crystal structure and a study of their antitumoral, antimicrobial and antiviral activities

机译:Pt(II)和Ag(I)与乙磺胺的配合物:晶体结构及其抗肿瘤,抗微生物和抗病毒活性的研究

摘要

Two new complexes of platinum(II) and silver(I) with acesulfame were synthesized. Acesulfame is in the anionic form acesulfamate (ace). The structures of both complexes were determined by X-ray crystallography. For K(2)[PtCl(2)(ace)(2)] the platinum atom is coordinated to two Cl(-) and two N-acesulfamate atoms forming a trans-square planar geometry. Each K(+) ion interacts with two oxygen atoms of the S(=O)(2) group of each acesulfamate. For the polymeric complex [Ag(ace)](n) the water molecule bridges between two crystallographic equivalent Agl atoms which are related each other by a twofold symmetry axis. Two Agl atoms, related to each other by a symmetry centre, make bond contact with two equivalent oxygen atoms. These bonds give rise to infinite chains along the unit cell diagonal in the ac plane. The in vitro cytotoxic analyses for the platinum complex using HeLa (human cervix cancer) cells show its low activity when compared to the vehicle-treated cells. The Ag(I) complex submitted to in vitro antimycobacterial tests, using the Microplate Alamar Blue (MABA) method, showed a good activity against Mycobacterium tuberculosis, responsible for tuberculosis, with a minimal inhibitory concentration (MIC) value of 11.6 mu M. The Ag(I) complex also presented a promising activity against Gram negative (Escherichia colt and Pseudomonas aeruginosa) and Gram positive (Enterococcus faecalis) microorganisms. The complex K(2)[PtCl(2)(ace)(2)] was also evaluated for antiviral properties against dengue virus type 2 (New Guinea C strain) in Vero cells and showed a good inhibition of dengue virus type 2 (New Guinea G strain) replication at 200 mu M, when compared to vehicle-treated cells. (C) 2010 Elsevier Inc. All rights reserved.
机译:合成了两个新的铂(II)和银(I)与乙酰磺胺的配合物。乙磺胺为乙酰氨基磺酸盐(ace)的阴离子形式。两种配合物的结构均通过X射线晶体学测定。对于K(2)[PtCl(2)(ace)(2)],铂原子与两个Cl(-)和两个N-乙酰氨基磺酸原子配位,形成一个方形的方形几何结构。每个K(+)离子与每个乙酰氨基磺酸S(= O)(2)基团的两个氧原子相互作用。对于聚合物配合物[Ag(ace)](n),水分子在两个晶体学等效Agl原子之间架桥,这两个原子通过双对称轴相互关联。通过对称中心彼此相关的两个Ag1原子与两个等效的氧原子进行键接触。这些键沿ac平面的对角线单位产生无限链。与载体处理的细胞相比,使用HeLa(人宫颈癌)细胞对铂复合物进行的体外细胞毒性分析显示其活性较低。使用Microplate Alamar Blue(MABA)方法进行体外抗分枝杆菌测试的Ag(I)复合物显示出对引起结核病的结核分枝杆菌具有良好的活性,最低抑制浓度(MIC)值为11.6μM. Ag(I)复合物还表现出对革兰氏阴性(大肠埃希氏菌和铜绿假单胞菌)和革兰氏阳性(粪肠球菌)的有希望的活性。还评估了复合物K(2)[PtCl(2)(ace)(2)]在Vero细胞中对2型登革热病毒(新几内亚C株)的抗病毒特性,并显示了对2型登革热病毒的良好抑制作用(新与媒介物处理过的细胞相比,几内亚G株)在200μM的速度复制。 (C)2010 Elsevier Inc.保留所有权利。

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