Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products
Yükleniyor...
Tarih
2012
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Taylor and Francis Ltd.
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
(2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl) methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl) benzene-1,2-diol (3), and 5,5'-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC50 values in the range of 0.7-372 mu M against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.
Açıklama
Anahtar Kelimeler
Bromophenols, Diphenylmethane, Carbonic anhydrase, Glaucoma, Enzyme inhibition
Kaynak
Journal of Enzyme Inhibition and Medicinal Chemistry
WoS Q Değeri
N/A
Scopus Q Değeri
Q1
Cilt
27
Sayı
1
Künye
Balaydın, H. T., Soyut, H., Ekinci, D., Göksu, S., Beydemir, Ş., Menzek, A., & Şahin, E. (2012). Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products. Journal of enzyme inhibition and medicinal chemistry, 27(1), 43-50.
