Some pyrazoles derivatives: Potent carbonic anhydrase, -glycosidase, and cholinesterase enzymes inhibitors


Turkan F., Cetin A., Taslimi P., GÜLÇİN İ.

ARCHIV DER PHARMAZIE, vol.351, no.10, 2018 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 351 Issue: 10
  • Publication Date: 2018
  • Doi Number: 10.1002/ardp.201800200
  • Journal Name: ARCHIV DER PHARMAZIE
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase, enzyme inhibition, substituted pyrazol-4-yl-diazene, INCLUDING NATURAL-PRODUCTS, GLUTATHIONE-S-TRANSFERASE, ALPHA-GLUCOSIDASE, 1ST SYNTHESIS, ACETYLCHOLINESTERASE, BUTYRYLCHOLINESTERASE, PROFILES, ANTIOXIDANT, BROMOPHENOLS, BENZENESULFONAMIDES
  • Van Yüzüncü Yıl University Affiliated: No

Abstract

A series of substituteed pyrazol-4-yl-diazene derivatives were found to be effective inhibitors against -glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with K-i values in the range of 33.72 +/- 7.93 to 90.56 +/- 27.52nM for -glycosidase, 1.06 +/- 0.16 to 9.83 +/- 0.74nM for hCA I, 0.68 +/- 0.12 to 7.16 +/- 1.14nM for hCA II, 44.66 +/- 10.06 to 78.34 +/- 17.83nM for AChE, and 50.36 +/- 13.88 to 88.36 +/- 20.03nM for BChE, respectively. Recently, inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances, such as diabetes, glaucoma, obesity, epilepsy, cancer, and neurodegenerative diseases.