Premium
Inhibition of paraoxonase 1 by coumarin‐substituted N‐heterocyclic carbene silver(I), ruthenium(II) and palladium(II) complexes
Author(s) -
Karataş Mert Olgun,
Çalgın Gamze,
Alıcı Bülent,
Gökçe Başak,
Gençer Nahit,
Taşkın Tok Tuğba,
Arslan Oktay,
KılıçCıkla Işın,
Özdemir Namık
Publication year - 2019
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/aoc.5130
Subject(s) - chemistry , palladium , ruthenium , carbene , coumarin , medicinal chemistry , stereochemistry , docking (animal) , crystal structure , organic chemistry , catalysis , medicine , nursing
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 IC 50 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.