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In vitro Anti‐atherogenic Properties of N‐Heterocyclic Carbene Aurate(I) Compounds
ChemMedChem ( IF 3.4 ) Pub Date : 2018-11-27 , DOI: 10.1002/cmdc.201800601
Eleni Sioriki 1 , Ronan Lordan 2 , Fady Nahra 1 , Kristof Van Hecke 1 , Ioannis Zabetakis 2 , Steven P. Nolan 1, 3
Affiliation  

The anti‐atherogenic (anti‐inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2] (NHC=N‐heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet‐activating factor (PAF)‐induced platelet aggregation was probed. All complexes were found to possess anti‐aggregatory properties in vitro with [IPr*⋅H][AuCl2] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti‐inflammatory drugs.

中文翻译:

N-杂环金碳酸盐(I)化合物的体外抗动脉粥样硬化特性

研究了通式[ NHC· H] [AuCl 2 ](NHC = N-杂环卡宾)的各种aurate(I)盐的抗动脉粥样硬化(抗炎)特性。所述金酸酯易于合成并以分析纯的形式获得。此外,还探讨了这些化合物通过体外抑制血小板活化因子(PAF)诱导的血小板凝集而对动脉粥样硬化的生物学活性。发现所有复合物均具有体外抗聚集特性,其中[IPr *⋅H] [AuCl 2 ](6)是微摩尔浓度下最有效的PAF抑制剂。根据我们的发现,我们得出结论,这些简单组装的金酸酯是一种非常有前途的PAF抑制剂和抗炎药。
更新日期:2018-11-27
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