| Literature DB >> 35175415 |
Yeliz Kaya1, Ayşe Erçağ2, Yunus Zorlu3, Yeliz Demir4, İlhami Gülçin5.
Abstract
Pd(II) complexes (Pd1, Pd2, and Pd3) were synthesized for the first time using asymmetric isatin bisthiocarbohydrazone ligands and PdCl2(PPh3)2. All complexes were characterized by a range of spectroscopic and analytical techniques. The molecular structures of Pd1 and Pd3 have been determined by single-crystal X-ray diffraction analysis. The complexes are diamagnetic and exhibit square planar geometry. The asymmetric isatin bisthiocarbohydrazone ligands coordinate to Pd(II) ion in a tridentate manner, through the phenolic oxygen, imine nitrogen and thiol sulfur, forming five- and six-membered chelate rings within their structures. The fourth coordination site in these complexes is occupied by PPh3 (triphenylphosphine). The free ligands and their Pd(II) complexes were evaluated for their carbonic anhydrase I, II (hCAs) and acetylcholinesterase (AChE) inhibitor activities. They showed a highly potent inhibition effect on AChE and hCAs. Ki values are in the range of 9 ± 0.6 - 30 ± 5.4 nM for AChE, 7 ± 0.5 - 16 ± 2.2 nM for hCA I and 3 ± 0.3-24 ± 1.9 nM for hCA II isoenzyme. The results clearly demonstrated that the ligands and their Pd(II) complexes effectively inhibited the used enzymes.Entities:
Keywords: Acetylcholinesterase; Bisthiocarbohydrazone; Carbonic anhydrase; Crystal structure; Isatin; Palladium(II)
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Year: 2022 PMID: 35175415 DOI: 10.1007/s00775-022-01932-9
Source DB: PubMed Journal: J Biol Inorg Chem ISSN: 0949-8257 Impact factor: 3.358