In vitro inhibition of human erythrocyte glutathione reductase by some new organic nitrates

Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are th...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (13), p.3661-3663
Hauptverfasser: Şentürk, Murat, Talaz, Oktay, Ekinci, Deniz, Çavdar, Hüseyin, Küfrevioğlu, Ömer İrfan
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Sprache:eng
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Zusammenfassung:Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to be useful for the treatment of malaria. Twelve organic nitrate derivatives were synthesized and treated with human erythrocyte GR. The molecules were identified as strong GR inhibitors and novel antimalaria candidates. Glutathione reductase (GR), is responsible for the existence of GSH molecule, a crucial antioxidant against oxidative stress reagents. The antimalarial activities of some redox active compounds are attributed to their inhibition of antioxidant flavoenzyme glutathione reductase, and inhibitors are therefore expected to be useful for the treatment of malaria. Twelve organic nitrate derivatives were synthesized and treated with human erythrocyte GR. The molecules were identified as strong GR inhibitors and novel antimalaria candidates.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.04.087