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Synthesis and Biological Studies of Novel Aminophosphonates and Their Metal Carbonyl Complexes (Fe, Ru).

ABSTRACT: The quest to find new inhibitors of biologically relevant targets is considered an important strategy to introduce new drug candidates for the treatment of neurodegenerative diseases. A series of (aminomethyl)benzylphosphonates 8a-c and their metallocarbonyl iron 9a-c and ruthenium 10a-c complexes were designed, synthesized, and evaluated for their inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) by determination of IC₅₀. Metallocarbonyl derivatives, in general, did not show significant inhibition activity against these enzymes, the most potent inhibitor was the (aminomethyl)benzylphosphonate 8a (IC₅₀ = 1.215 µM against AChE). Molecular docking analysis of AChE and (aminomethyl)benzylphosphonates 8a-c showed the strongest interactions of 8a and AChE compared to isomers 8b and 8c. Cytotoxicity studies of synthesized compounds towards the V79 cell line were also performed and discussed.

SUBMITTER: Kosinska A

PROVIDER: S-EPMC9330042 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature

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Synthesis and Biological Studies of Novel Aminophosphonates and Their Metal Carbonyl Complexes (Fe, Ru).

Kosińska Aneta A Virieux David D Pirat Jean-Luc JL Czarnecka Kamila K Girek Małgorzata M Szymański Paweł P Wojtulewski Sławomir S Vasudevan Saranya S Chworos Arkadiusz A Rudolf Bogna B

International journal of molecular sciences 20220722 15

The quest to find new inhibitors of biologically relevant targets is considered an important strategy to introduce new drug candidates for the treatment of neurodegenerative diseases. A series of (aminomethyl)benzylphosphonates 8a-c and their metallocarbonyl iron 9a-c and ruthenium 10a-c complexes were designed, synthesized, and evaluated for their inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) by determinatio ...[more]

PMID: 35897660

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Dataset Information

Synthesis and Biological Studies of Novel Aminophosphonates and Their Metal Carbonyl Complexes (Fe, Ru).

Publications

Synthesis and Biological Studies of Novel Aminophosphonates and Their Metal Carbonyl Complexes (Fe, Ru).

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