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

Napredna pretraga

Pregled bibliografske jedinice broj: 1209470

Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase


Elsinghorst, Paul W.; Wille, Timo; Barić, Danijela; Mertens, Matthias. D.; Baumann, Madlen; Küppers, Jim; Gütschow, Michael
Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase // Archiv der pharmazie, 355 (2022), e2200208, 11 doi:10.1002/ardp.202200208 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1209470 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase

Autori
Elsinghorst, Paul W. ; Wille, Timo ; Barić, Danijela ; Mertens, Matthias. D. ; Baumann, Madlen ; Küppers, Jim ; Gütschow, Michael

Izvornik
Archiv der pharmazie (0365-6233) 355 (2022); E2200208, 11

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
acetylcholinesterase, coumarins, enzyme reactivation, Mitsunobu reaction, organophosphorus compounds

Sažetak
Reactivation of inhibited acetylcholinesterase remains an important therapeutic strategy for the treatment of poisoning by organophosphorus compounds, such as nerve agents or pesticides. Although drugs like obidoxime or pralidoxime have been used with considerable success, there is a need for new substances capable of reactivating acetylcholinesterase with a broader scope and increased efficacy. Possible screening candidates must fulfill two fundamental requirements: They must (i) show an affinity to acetylcholinesterase well balanced between sufficient binding and competitive inhibition and (ii) facilitate the nucleophilic cleavage of the phosphorylated catalytic serine residue. We attached a variety of nonaromatic primary and secondary amines to a coumarin core through selected alkoxy side linkers attached at coumarin positions 6 or 7 to obtain a small set of possible reactivators. Evaluation of their inhibition and reactivation potential in vitro showed some activity with respect to acetylcholinesterase inhibited by cyclosarin.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija



POVEZANOST RADA


Ustanove:
Institut "Ruđer Bošković", Zagreb

Profili:

Avatar Url Danijela Barić (autor)

Poveznice na cjeloviti tekst rada:

doi onlinelibrary.wiley.com

Citiraj ovu publikaciju:

Elsinghorst, Paul W.; Wille, Timo; Barić, Danijela; Mertens, Matthias. D.; Baumann, Madlen; Küppers, Jim; Gütschow, Michael
Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase // Archiv der pharmazie, 355 (2022), e2200208, 11 doi:10.1002/ardp.202200208 (međunarodna recenzija, članak, znanstveni)
Elsinghorst, P., Wille, T., Barić, D., Mertens, M., Baumann, M., Küppers, J. & Gütschow, M. (2022) Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase. Archiv der pharmazie, 355, e2200208, 11 doi:10.1002/ardp.202200208.
@article{article, author = {Elsinghorst, Paul W. and Wille, Timo and Bari\'{c}, Danijela and Mertens, Matthias. D. and Baumann, Madlen and K\"{u}ppers, Jim and G\"{u}tschow, Michael}, year = {2022}, pages = {11}, DOI = {10.1002/ardp.202200208}, chapter = {e2200208}, keywords = {acetylcholinesterase, coumarins, enzyme reactivation, Mitsunobu reaction, organophosphorus compounds}, journal = {Archiv der pharmazie}, doi = {10.1002/ardp.202200208}, volume = {355}, issn = {0365-6233}, title = {Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase}, keyword = {acetylcholinesterase, coumarins, enzyme reactivation, Mitsunobu reaction, organophosphorus compounds}, chapternumber = {e2200208} }
@article{article, author = {Elsinghorst, Paul W. and Wille, Timo and Bari\'{c}, Danijela and Mertens, Matthias. D. and Baumann, Madlen and K\"{u}ppers, Jim and G\"{u}tschow, Michael}, year = {2022}, pages = {11}, DOI = {10.1002/ardp.202200208}, chapter = {e2200208}, keywords = {acetylcholinesterase, coumarins, enzyme reactivation, Mitsunobu reaction, organophosphorus compounds}, journal = {Archiv der pharmazie}, doi = {10.1002/ardp.202200208}, volume = {355}, issn = {0365-6233}, title = {Aminoalkoxy-substituted coumarins: Synthesis and evaluation for reactivation of inhibited human acetylcholinesterase}, keyword = {acetylcholinesterase, coumarins, enzyme reactivation, Mitsunobu reaction, organophosphorus compounds}, chapternumber = {e2200208} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


Citati:





    Contrast
    Increase Font
    Decrease Font
    Dyslexic Font