SYNTHESIS AND BIOLOGICAL EVALUATION OF UNUSUAL ALPHA-AMINO ACIDS FOR BIOMEDICAL STRATEGIES.

Autor: SIMONYAN, HAYARPI, ROVIELLO, GIOVANNI N., EWERT, ERNEST, FIK-JASKÓŁKA, MARTA, MKRTCHYAN, ANNA
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Zdroj: Medical Science Pulse; 2024 Supplement, Vol. 18, p29-29, 1p
Abstrakt: Introduction: Unusual amino acids play vital roles in biology, serving as bioactive molecules, scaffolds, and building blocks for drug discovery. The asymmetric synthesis of chiral molecules, especially amino acids, is crucial in pharmaceutical research due to the distinct behaviour of individual enantiomers. Aim: This study aims to asymmetrically synthesize a novel class of enantiomerically enriched α-amino acids with heterocyclic substituents in the side-chain radical. We seek to investigate their biological activity and potential applications in drug delivery systems. Material and methods: Using a chiral niII complex of Schiff's base derived from dehydroalanine and dehydroamonobutyric acid, along with the chiral auxiliary (S)-2-n-(n'-benzylprolyl)aminobenzo-phenone, we synthesized amino acids with high optical purity (ee>95%). Biological examination involved UV analysis, fluorescence studies, dynamic light scattering (DLS), molecular docking, and cell vitality assays. Results: Our findings reveal the significant impact of synthesised amino acids on alpha-helix formation, supramolecular networks, and structural changes in serum albumin, as elucidated through CD and UV (HT(V)) spectra. Molecular docking highlighted unique subdomain interactions, showcasing diverse modulatory effects on serum albumin. Conclusions: This study lays the foundation for further exploration into protein-drug interactions and the development of innovative drug delivery systems. The potential of artificial amino acids offers promising avenues for patient-centric therapies and advancements in pharmaceutical research. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index