Pretražite po imenu i prezimenu autora, mentora, urednika, prevoditelja

Napredna pretraga

Pregled bibliografske jedinice broj: 1124853

Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system


Matošević, Ana; Bosak, Anita
Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system // Knjiga sažetaka 5.Simpozija studenata doktorskih studija PMF-a / Barišić, Dajana (ur.).
Zagreb: Prirodoslovno-matematički fakultet, Sveučilište u Zagrebu, 2021. str. 146-146 (poster, domaća recenzija, sažetak, znanstveni)


CROSBI ID: 1124853 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system

Autori
Matošević, Ana ; Bosak, Anita

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Knjiga sažetaka 5.Simpozija studenata doktorskih studija PMF-a / Barišić, Dajana - Zagreb : Prirodoslovno-matematički fakultet, Sveučilište u Zagrebu, 2021, 146-146

ISBN
978-953-6076-90-1

Skup
5. Simpozij studenata doktorskih studija PMF-a

Mjesto i datum
Zagreb, Hrvatska, 24-25.04.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
neurodegenerative diseases ; cholinseterases ; carbamates ; 4-aminoquinolines

Sažetak
Nervous system diseases are caused by the gradual and progressive death of neurons, which in turn leads to dysfunctions of the nervous system and causes problems in the mental and physical functioning of patients. Alzheimer's (AD) and Parkinson's disease and myasthenia gravis are complex neurological disorders currently treated with drugs that inhibit the activity of acetylcholine hydrolyzing enzymes (acetylcholinesterase and butyrylcholinesterase) or are N-methyl-D- aspartate receptor antagonists. However, these drugs act only on the symptoms, not on the course and outcome of the disease. As these are diseases whose development and progression are affected by multiple pathological factors, the pharmaceutical industry and the scientific community have recently made great efforts to find new effective drugs, with a tendency to replace current "single-targeted" drugs with those that act on multi targets – “multi- target-directed ligands” (MTDL). The primary goal of the HRZZ project IP-2020- 02-9343 "Development of bioactive molecules for the treatment of neurodegenerative diseases" is the development of MTDL compounds with the potential to alleviate symptoms and slow down the progression of ND (especially AD). The development of such compounds will have two main goals: the development of compounds active in the central nervous system (CNS) and the development of peripherally active compounds, depending on their ability to cross the blood- brain barrier. Part of the research is focused on the design and synthesis of biscarbamate compounds, structural analogues of resorcinol, as potential cholinesterase's inhibitors. To date, four groups of compounds with different aliphatic and cyclic substituents in the carbamoyl and amino parts of the molecule have been synthesized. Compounds of appropriate purity (>97%) were kinetically evaluated as human cholinesterase inhibitors and proven to be fast inhibitors of both cholinesterases with inhibition rate constants within 106 M-1 min-1. In addition, the tested compounds showed no toxic effect on liver and neuroblastoma cells at concentrations showing an inhibitory effect on cholinesterases, and some were estimated to be able to cross the blood-brain barrier by active transport. The obtained results will enable the definition of guidelines for structural refining of compounds that could be more effective in the treatment of ND than the currently available drugs.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija



POVEZANOST RADA


Projekti:
HRZZ-IP-2020-02-9343 - Razvoj bioaktivnih molekula za tretman neurodegenerativnih bolesti (BioMol4ND) (Bosak, Anita, HRZZ - 2020-02) ( POIROT)

Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb

Profili:

Avatar Url Ana Matošević (autor)

Avatar Url Anita Bosak (autor)


Citiraj ovu publikaciju

Matošević, Ana; Bosak, Anita
Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system // Knjiga sažetaka 5.Simpozija studenata doktorskih studija PMF-a / Barišić, Dajana (ur.).
Zagreb: Prirodoslovno-matematički fakultet, Sveučilište u Zagrebu, 2021. str. 146-146 (poster, domaća recenzija, sažetak, znanstveni)
Matošević, A. & Bosak, A. (2021) Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system. U: Barišić, D. (ur.)Knjiga sažetaka 5.Simpozija studenata doktorskih studija PMF-a.
@article{article, editor = {Bari\v{s}i\'{c}, D.}, year = {2021}, pages = {146-146}, keywords = {neurodegenerative diseases, cholinseterases, carbamates, 4-aminoquinolines}, isbn = {978-953-6076-90-1}, title = {Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system}, keyword = {neurodegenerative diseases, cholinseterases, carbamates, 4-aminoquinolines}, publisher = {Prirodoslovno-matemati\v{c}ki fakultet, Sveu\v{c}ili\v{s}te u Zagrebu}, publisherplace = {Zagreb, Hrvatska} }
@article{article, editor = {Bari\v{s}i\'{c}, D.}, year = {2021}, pages = {146-146}, keywords = {neurodegenerative diseases, cholinseterases, carbamates, 4-aminoquinolines}, isbn = {978-953-6076-90-1}, title = {Design, synthesis and biological evaluation of compounds as active drugs in the central and peripheral nervous system}, keyword = {neurodegenerative diseases, cholinseterases, carbamates, 4-aminoquinolines}, publisher = {Prirodoslovno-matemati\v{c}ki fakultet, Sveu\v{c}ili\v{s}te u Zagrebu}, publisherplace = {Zagreb, Hrvatska} }




Contrast
Increase Font
Decrease Font
Dyslexic Font