Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols and their derivatives including natural products: Vidalol B


Balaydin H. T., SENTURK M., GÖKSU S., MENZEK A.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.54, ss.423-428, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 54
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1016/j.ejmech.2012.05.025
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.423-428
  • Anahtar Kelimeler: Phenol, Bromination, Bromophenols, Diphenylmethane, Carbonic anhydrase, Glaucoma, Enzyme inhibition, Vidalol A, Vidalol B, ALGA SYMPHYOCLADIA-LATIUSCULA, THERAPEUTIC APPLICATIONS, ODONTHALIA-CORYMBIFERA, VI, ISOZYMES, PHENOLS, ACTIVATORS
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Hayır

Özet

A series of bisphenol, bromophenol, and methoxyphenol derivatives (2-24) including the natural bromophenols vidalol B, 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (2) and 5,5'-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (3) were prepared. In the current study, inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, I, II, IV, and VI, with these compounds 2-24 was investigated. The compounds 2-24 were found to be promising carbonic anhydrase inhibitors, some of which showed interesting inhibitory activities. Some of the compounds investigated here showed effective hCA 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, and osteoporosis. (C) 2012 Elsevier Masson SAS. All rights reserved.