Sioriki, E;Lordan, R;Nahra, F;van Hecke, K;Zabetakis, I;Nolan, SP

2018

December

Chemmedchem

In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds

Published

11 ()

PLATELET-ACTIVATING-FACTOR FACTOR PAF RECEPTOR POTENT INFLAMMATION ANTAGONIST HISTAMINE DISEASE ATHEROSCLEROSIS METASTASIS

13

2484

2487

The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC center dot 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*center dot 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.

WEINHEIM

1860-7179

10.1002/cmdc.201800601