Some coumarins and benzoxazinones as potent paraoxonase 1 inhibitors

Basit Öğe Kaydı
dc.authoridTR120424en_US
dc.authoridTR38542en_US
dc.authoridTR6993en_US
dc.authoridTR120204en_US
dc.authoridTR29091en_US
dc.authoridTR5067en_US
dc.authoridTR38542en_US
dc.contributor.authorKarataş, Mert Olgun
dc.contributor.authorAlıcı, Bülent
dc.contributor.authorGökçe, Başak
dc.contributor.authorGencer, Nahit
dc.contributor.authorArslan, Oktay
dc.contributor.authorUslu, Harun
dc.date.accessioned2017-04-12T08:31:51Z
dc.date.available2017-04-12T08:31:51Z
dc.date.issued2016
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, we aimed to investigate the effect of some coumarin and benzoxazinone derivatives on the activity of human PON1. Human serum paraoxonase 1 was purified from fresh human serum blood by two-step procedures that are ammonium sulfate precipitation (60–80%) and then hydrophobic interaction chromatography (Sepharose 4B, L-tyrosine and 1-napthylamine). The enzyme was purified 232-fold with a final specific activity of 27.1 U/mg. In vitro effects of some previously synthesized ionic coumarin or benzoxazinone derivatives (1–21) on purified PON1 activity were investigated. Compound 14 (1-(2,3,4,5,6)-pentamethylbenzyl-3-(6,8-dimethyl-2H-chromen-2-one-4-yl))benzimidazolium chloride was found out as the strongest inhibitor (IC50 ¼ 7.84 mM) for PON1 among the compounds. Kinetic investigation and molecular docking study were evaluated for one of the most active compounds (compound 12) and obtained data showed that this compound is competitive inhibitor of PON1 and interact with Leu262 and Ser263 in the active site of PON1. Moreover, coumarin derivatives were found out as the more potent inhibitors for PON1 than benzoxazinone derivativesen_US
dc.identifier.citationKarataş, M. O. Alıcı, B. Gökçe, B. Gencer, N. Arslan, O. Uslu, H. (2016). Some coumarins and benzoxazinones as potent paraoxonase 1 inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, 31(6), 1386–1391.en_US
dc.identifier.doi10.3109/14756366.2016.1142982en_US
dc.identifier.endpage1391en_US
dc.identifier.issn1475-6366
dc.identifier.issue6en_US
dc.identifier.startpage1386en_US
dc.identifier.urihttps://www.tandfonline.com/doi/full/10.3109/14756366.2016.1142982
dc.identifier.urihttps://hdl.handle.net/11616/6646
dc.identifier.volume31en_US
dc.language.isoenen_US
dc.publisherJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectBenzoxazinoneen_US
dc.subjectCoumarinen_US
dc.subjectDockingen_US
dc.subjectInhibitionen_US
dc.subjectParaoxonaseen_US
dc.titleSome coumarins and benzoxazinones as potent paraoxonase 1 inhibitorsen_US
dc.typeArticleen_US

Dosyalar

Orijinal paket
Listeleniyor 1 - 1 / 1
Küçük Resim
İsim:
Makale Dosyası.pdf
Boyut:
844.45 KB
Biçim:
Adobe Portable Document Format
Açıklama:
Makale Dosyası
İndir
Lisans paketi
Listeleniyor 1 - 1 / 1
Küçük Resim Yok
İsim:
license.txt
Boyut:
1.71 KB
Biçim:
Item-specific license agreed upon to submission
Açıklama:
İndir

Koleksiyon

Sağlık Bilimleri Enstitüsü Diğer Yayınlar Koleksiyonu