A simple O-sulfated thiohydroximate molecule to be the first micromolar range myrosinase inhibitor

A simple O-sulfated thiohydroximate molecule to be the first micromolar range myrosinase inhibitor

New non-hydrolyzable analogues of glucosinolates have been prepared. Myrosinase inhibition was observed with modified aglycon moieties, even bulky phenothiazine analogue 6 gave reasonable inhibition. The simplest structure 8 derived from dimethylaminoethanethiol has shown to be the most potent inhib...

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Veröffentlicht in:Tetrahedron letters 2009-07, Vol.50 (26), p.3302-3305
Hauptverfasser: Cerniauskaite, Deimante, Gallienne, Estelle, Karciauskaite, Henreta, Farinha, Andrea S.F., Rousseau, Jolanta, Armand, Sylvie, Tatibouët, Arnaud, Sackus, Algirdas, Rollin, Patrick
Format: Artikel
Sprache:eng
Schlagworte:
Glucosinolate
Myrosinase inhibition
Sulfation
Thiohydroximate
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Zusammenfassung:New non-hydrolyzable analogues of glucosinolates have been prepared. Myrosinase inhibition was observed with modified aglycon moieties, even bulky phenothiazine analogue 6 gave reasonable inhibition. The simplest structure 8 derived from dimethylaminoethanethiol has shown to be the most potent inhibitor with an IC 50 of 3.32 μM.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2009.02.072