Návrh štruktúry, syntéza a biologická aktivita nových karbamátových inhibítorov cholínesteráz

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  • Lucia Ungvarská Maľučká Katedra chémie, biochémie a biofyziky, Univerzita veterinárskeho lekárstva a farmácie v Košiciach, Košice, Slovenská republika | Ústav chemických léčiv, Farmaceutická fakulta, Masarykova univerzita, Brno, Česká republika https://orcid.org/0000-0003-1119-9564
  • Jozef Csöllei Ústav chemických léčiv, Farmaceutická fakulta, Masarykova univerzita, Brno, Česká republika https://orcid.org/0000-0002-1147-4784

DOI:

https://doi.org/10.54779/chl20220372

Klíčová slova:

acetylcholínesteráza, butyrylcholínesteráza, syntéza, nové inhibítory, karbamátové deriváty, multifunkčne zamerané látky

Abstrakt

The work deals with the design, synthesis and biological activity of new carbamate cholinesterase inhibitors. It is focused on selected syntheses of new carbamate derivatives, which were tested for their anticholinesterase activity against acetylcholinesterase as well as butyrylcholinesterase. Despite various theories in the pathogenesis of Alzheimer's disease, drugs that can inhibit these two enzymes still represent the major approach to the treatment of this neurodegenerative disease. Many of the newly synthesized compounds have unique chemical structure. Recently, the approach to the synthesis of new cholinesterase inhibitors has focused on the preparation of potential drugs, containing in their chemical structure fragments of already known drugs, commonly used in the pharmacotherapy of Alzheimer's disease, but also other diseases. The aim of preparing these compounds is to affect several biological systems simultaneously. These multipotent compounds have been termed "multi-target-directed ligands"; the molecules of drugs used to treat Alzheimer's disease always contain a pharmacophore acting as a cholinesterase inhibitor, which represents the mainstay of therapy.

Stahování

Publikováno

15.06.2022

Jak citovat

Ungvarská Maľučká, L., & Csöllei, J. (2022). Návrh štruktúry, syntéza a biologická aktivita nových karbamátových inhibítorov cholínesteráz. Chemické Listy, 116(6), 372–380. https://doi.org/10.54779/chl20220372

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