Inhibition of paraoxonase 1 by coumarin‐substituted N‐heterocyclic carbene silver(I), ruthenium(II) and palladium(II) complexes |
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Authors: | Mert Olgun Karata Gamze algn Bülent Alc Baak Gke Nahit Gener Tuba Takn Tok Oktay Arslan In Kl‐Ckla Namk
zdemir |
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Institution: | Mert Olgun Karata?,Gamze Çalg?n,Bülent Al?c?,Ba?ak Gökçe,Nahit Gençer,Tu?ba Ta?k?n Tok,Oktay Arslan,I??n K?l?ç‐C?kla,Nam?k Özdemir |
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Abstract: | We synthesized three coumarin‐substituted benzimidazolium chlorides and their silver(I), ruthenium(II) and palladium(II) N‐heterocyclic carbene (NHC) complexes. All compounds were characterized using appropriate spectroscopic techniques and elemental analyses. Single‐crystal X‐ray structure of a Pd(II)–NHC complex ( 6b ) was also determined. The inhibitory properties of all compounds were tested on the activity of human paraoxonase 1 (PON1). All complexes exhibited weaker inhibitory properties than their corresponding benzimidazolium salts except for complex 6b which is the most active inhibitor with an IC50 value of 3.01 μM among the compounds reported in this study. A kinetic evaluation showed that this complex inhibits PON1 activity in a non‐competitive manner. Molecular docking studies were also performed for 6b in order to obtain more insight into the binding mode. |
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Keywords: | coumarin inhibition N‐heterocyclic carbenes paraoxonase 1 |
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