SYNTHESIS AND INHIBITORY POTENTIAL OF UGI PRODUCTS TOWARDS BUTYRYLCHOLINESTERASE

Abstract

In this work, we have synthesized a series of structurally related peptide-like compounds through the Ugi reaction by using different N-tert-butyloxycarbonyl (Boc) protected amino acids or benzoic acid with formaldehyde / acetone, benzylamine / isobutylamine and tert-butyl / benzyl isocyanide. All compounds were synthesized by classical organic synthesis methods and by microwave-assisted organic synthesis. The structure of all prepared compounds was determined by spectroscopic (1D and 2D 1H and 13C nuclear magnetic resonance spectroscopy) and spectrometric (high-resolution mass spectrometry) methods. The inhibitory potential of all prepared compounds towards the enzyme butyrylcholinesterase (BChE, E.C. 3.1.1.8.) isolated from horse serum was determined by the Ellman method

References

1. Ugi, I; Werner, B; Dцmling, A. Molecules 2003, 8, 56–66.
2. Lucía Campos-Prieto, Aitor García-Rey, Eddy Sotelo, Ana Mallo-Abreu. (2024). Multicomponent reactions driving the discovery and optimization of agents targeting central nervous system pathologies.Beilstein Journal of Organic Chemistry.[Crossref]
3. Alma Ramić, Toni Divjak, Lucija Hadrović, Matej Pavlinić, Ana Matošević, Anita Bosak, Jakov Borovec, Bruna Bakota, Tomica Hrenar, Ines Primožič. (2026). Cholinesterases inhibition profiles with Ugi-derived peptide­mimetics: A combined experimental and computational study.ADMET and DMPK.[Crossref]
4. George L. Ellman, K.Diane Courtney, Valentino Andres, Robert M. Featherstone. (1961). A new and rapid colorimetric determination of acetylcholinesterase activity.Biochemical Pharmacology.[Crossref]

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