Coumarin or benzoxazinone based novel carbonic anhydrase inhibitors synthesis molecular docking and anticonvulsant studies
Yükleniyor...
Dosyalar
Tarih
2016
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Journal of Enzyme Inhibition and Medicinal Chemistry
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Among many others, coumarin derivatives are known to show human carbonic anhydrase
(hCA) inhibitory activity. Since hCA inhibition is one of the underlying mechanisms that account
for the activities of some antiepileptic drugs (AEDs), hCA inhibitors are expected to have antiseizure
properties. There are also several studies reporting compounds with an imidazole
and/or benzimidazole moiety which exert these pharmacological properties. In this study, we
prepared fifteen novel coumarin-bearing imidazolium and benzimidazolium chloride, nine
novel benzoxazinone-bearing imidazolium and benzimidazolium chloride derivatives and
evaluated their hCA inhibitory activities and along with fourteen previously synthesized
derivatives we scanned their anticonvulsant effects. As all compounds inhibited purified hCA
isoforms I and II, some of them also proved protective against Maximal electroshock seizure
(MES) and ScMet induced seizures in mice. Molecular docking studies with selected coumarin
derivatives have revealed that these compounds bind to the active pocket of the enzyme in a
similar fashion to that previously described for coumarin derivatives.
Açıklama
Anahtar Kelimeler
Anticonvulsant, Benzoxazinone, Carbonic anhydrase, Coumarin, Epilepsy, İnhibition
Kaynak
Journal of Enzyme Inhibition and Medicinal Chemistry
WoS Q Değeri
Scopus Q Değeri
Cilt
31
Sayı
5
Künye
Karataş, M. O. Uslu, H. Sarı, S. Alagöz, M. A. Karakurt, A. Alıcı, B. Bilen, Ç. Yavuz, E. Gençer, N. Arslan, O. (2016). Coumarin or benzoxazinone based novel carbonic anhydrase inhibitors synthesis molecular docking and anticonvulsant studies. Journal of Enzyme Inhibition and Medicinal Chemistry, 31(5), 760–772.
