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Pregled bibliografske jedinice broj: 883673

Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity


Bosak, Anita; Knežević, Anamarija; Gazić Smilović, Ivana; Šinko, Goran; Kovarik, Zrinka
Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity // Journal of enzyme inhibition and medicinal chemistry, 32 (2017), 1; 789-797 doi:10.1080/14756366.2017.1326109 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 883673 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity

Autori
Bosak, Anita ; Knežević, Anamarija ; Gazić Smilović, Ivana ; Šinko, Goran ; Kovarik, Zrinka

Izvornik
Journal of enzyme inhibition and medicinal chemistry (1475-6366) 32 (2017), 1; 789-797

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

Ključne riječi
acetylcholinesterase, butyrylcholinesterase, adrenaline, salmeterol, terbutaline

Sažetak
We investigated the influence of bronchodilating 2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrine as catechol derivatives, and salbutamol and salmeterol as saligenin derivatives. All of the tested compounds reversibly inhibited cholinesterases with Ki constants ranging from 9.8 µM to 6.4 mM, and had the highest inhibition potency toward usual BChE, but generally none of the cholinesterases displayed any stereoselectivity. Kinetic and docking results revealed that the inhibition potency of the studied compounds could be related to the size of the hydroxyaminoethyl chain on the benzene ring. The additional - interaction of salmeterol’s benzene ring and Trp286 and hydrogen bond with His447 probably enhanced inhibition by salmeterol which was singled out as the most potent inhibitor of all the cholinesterases.

Izvorni jezik
Engleski

Znanstvena područja
Temeljne medicinske znanosti, Javno zdravstvo i zdravstvena zaštita, Farmacija



POVEZANOST RADA


Projekti:
HRZZ-IP-2013-11-4307 - Dizajn, sinteza i evaluacija novih protuotrova kod trovanja živčanim bojnim otrovima i pesticidima (CHOLINESTERASE) (Kovarik, Zrinka, HRZZ - 2013-11) ( POIROT)

Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb,
Institut "Ruđer Bošković", Zagreb

Profili:

Avatar Url Goran Šinko (autor)

Avatar Url Ivana Gazić (autor)

Avatar Url Anita Bosak (autor)

Avatar Url Anamarija Knežević (autor)

Citiraj ovu publikaciju

Bosak, Anita; Knežević, Anamarija; Gazić Smilović, Ivana; Šinko, Goran; Kovarik, Zrinka
Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity // Journal of enzyme inhibition and medicinal chemistry, 32 (2017), 1; 789-797 doi:10.1080/14756366.2017.1326109 (međunarodna recenzija, članak, znanstveni)
Bosak, A., Knežević, A., Gazić Smilović, I., Šinko, G. & Kovarik, Z. (2017) Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity. Journal of enzyme inhibition and medicinal chemistry, 32 (1), 789-797 doi:10.1080/14756366.2017.1326109.
@article{article, year = {2017}, pages = {789-797}, DOI = {10.1080/14756366.2017.1326109}, keywords = {acetylcholinesterase, butyrylcholinesterase, adrenaline, salmeterol, terbutaline}, journal = {Journal of enzyme inhibition and medicinal chemistry}, doi = {10.1080/14756366.2017.1326109}, volume = {32}, number = {1}, issn = {1475-6366}, title = {Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity}, keyword = {acetylcholinesterase, butyrylcholinesterase, adrenaline, salmeterol, terbutaline} }
@article{article, year = {2017}, pages = {789-797}, DOI = {10.1080/14756366.2017.1326109}, keywords = {acetylcholinesterase, butyrylcholinesterase, adrenaline, salmeterol, terbutaline}, journal = {Journal of enzyme inhibition and medicinal chemistry}, doi = {10.1080/14756366.2017.1326109}, volume = {32}, number = {1}, issn = {1475-6366}, title = {Resorcinol-, catechol- and saligenin-based bronchodilating beta2-agonists as inhibitors of human cholinesterase activity}, keyword = {acetylcholinesterase, butyrylcholinesterase, adrenaline, salmeterol, terbutaline} }

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


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