engleski

Synthesis, photochemistry and biological activity of new 1,2,3-triazolostilbenes. An experimental and computational study

Triazoles present an important class of heterocyclic compounds exhibiting a wide range of pharmacological activities [1]. New 1, 2, 3- triazolostilbenes were synthesized and photochemically transformed to electrocyclization products in high yields for the purpose of studying their acetyl- and butyrylcholinesterase inhibition and anti-inflammatory activity [2]. In our previous paper [3], photoreactivity of 1, 2, 3- ditriazolostilbenes were investigated showing unreactivity toward the electrocyclization. In contrast, 1, 2, 3-triazolostilbenes gave electrocyclization photoproducts in high isolated yields providing especially interesting results on cholinesterase inhibition associated with the inhibition of TNFalpha cytokine production. Additionally, the electronic structure of the obtained 1, 2, 3-triazolostilbenes and the thermodynamic stability of the 1, 2, 3- triazolostilbenes - cholinesterases complexes were investigated by computer modeling. REFERENCES [1] O. Silakari, Molecules 2018, 9, 1-29. [2] S. Vakine, H. Soreq, Neuropharmacology 2020, 168, 108020. [3] A. Ratković, M. Mlakić, W. Dehaen, T. Opsomer, D. Barić, I. Škorić, Spectrochim acta A 2021, 261, 120056.

electrocyclization photoproducts ; cholinesterase inhibition, inhibition of TNFalpha cytokine production ; computer modeling

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