Design, Synthesis and Biological Activity of New Carbamate Cholinesterase Inhibitors

Authors

  • Lucia Ungvarská Maľučká Department of Chemistry, Biochemistry and Biophysics, University of Veterinary Medicine and Pharmacy in Košice, Košice, Slovak Republic | Department of Chemical Drugs, Faculty of Pharmacy, Masaryk University, Brno, Czech Republic https://orcid.org/0000-0003-1119-9564
  • Jozef Csöllei Department of Chemical Drugs, Faculty of Pharmacy, Masaryk University, Brno, Czech Republic https://orcid.org/0000-0002-1147-4784

DOI:

https://doi.org/10.54779/chl20220372

Keywords:

acetylcholinesterase, butyrylcholinesterase, synthesis, new inhibitors, carbamate derivatives, multi-target directed ligands

Abstract

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.

Published

2022-06-15

How to Cite

Ungvarská Maľučká, L., & Csöllei, J. (2022). Design, Synthesis and Biological Activity of New Carbamate Cholinesterase Inhibitors. Chemické Listy, 116(6), 372–380. https://doi.org/10.54779/chl20220372

Issue

Section

Articles