Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes      
Yazarlar (5)
Ümit Muhammet Koçyiğit
Cumhuriyet Üniversitesi, Türkiye
Parham Taslimi
Hayreddin Gezegen
Cumhuriyet Üniversitesi, Türkiye
İlhami Gülçin
Atatürk Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
Dergi ISSN 1095-6670 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q4
Makale Dili İngilizce
Basım Tarihi 09-2017
Cilt No 31
Sayı 9
Sayfalar 21938 / 0
DOI Numarası 10.1002/jbt.21938
Makale Linki http://doi.wiley.com/10.1002/jbt.21938
Özet
Carbonic anhydrase (CA; EC 4.2.1.1) is used for remedial purposes for several years, as there is significant focus on expanding more new activators (CAAs) and high affinity inhibitors. Alzheimer's disease and other similar ailments such as dementia and vascular dementia with Lewy bodies reduce cholinergic activity in the important areas involved in cognition and memory. Prevalent drugs for the symptomatic therapy of dementia are significant in increasing the associated cholinergic deficiency by inhibiting acetylcholinesterase (AChE). These six-membered carbocycles showed nice inhibitory action against AChE and human carbonic anhydrase (hCA) II and I isoforms. The hCA I, II, and AChE were efficiently inhibited by these molecules, with K values in the range of 6.70-35.85 nM for hCA I, 18.77-60.84 nM for hCA II, and 0.74-4.60 for AChE, respectively.
Anahtar Kelimeler
acetylcholinesterase | carbonic anhydrase | domino reactions | enzyme inhibition pentasubstituted cyclohexanol