Published January 1, 2021
| Version v1
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New silver N-heterocyclic carbenes complexes: Synthesis, molecular docking study and biological activities evaluation as cholinesterase inhibitors and antimicrobials
Creators
- 1. Abd el Hafid Boussouf Mila Univ Ctr, Inst Sci & Technol, Dept Tech Sci, Mila 43000, Algeria
- 2. Mentouri Constantine 1 Univ, Fac Nat & Life Sci, Dept Biochem & Cellular & Mol Biol, Lab Appl Biochem, Constantine 25000, Algeria
- 3. Biotechnol Res Ctr, Constantine 25000, Algeria
- 4. Inonu Univ, Fac Sci & Art, Dept Mol Biol & Genet, TR-44280 Malatya, Turkey
- 5. Inonu Univ, Med Sch, Dept Med Biol & Genet, Malatya, Turkey
- 6. Inonu Univ, Catalysis Res & Applicat Ctr, TR-44280 Malatya, Turkey
- 7. Mentouri Constantine 1 Univ, Fac Exact Sci, Lab Synth Mol Biol Interest, Constantine 25000, Algeria
Description
We focused our study for the conception and the synthesis of a new series of Silver (I) N-heterocyclic carbene complexes which were obtained from the corresponding N-heterocyclic carbene (NHC) precursors and their unsymmetrical benzimidazolium salts. These new Ag-NHC complexes were screened for their antibacterial, antifungal, and anti-cholinesterase activities. The biological activities of synthesized products were compared with standard drugs. N-heterocyclic carbenes 2a-f and complexes 3a-f exhibited moderate antibacterial and antifungal activities. The results proved that the compounds indicated moderate to excellent activity against both AChE and BuChE. It was found that most of the complexes displayed good AChE and BuChE inhibitory activities. In particular, compounds 3c and 3e were the most potent inhibitors in the series with IC50 values of 8.56 +/- 1.17 mu M and 5.05 +/- 0.30 mu M against AChE and BChE, respectively. Docking studies revealed that compounds 3c and 3e bind manly to the catalytic anionic site (CAS) of the AChE, and BChE respectively. (C) 2021 Elsevier B.V. All rights reserved.
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