| Literature DB >> 30769267 |
Fikret Turkan1, Adnan Cetin2, Parham Taslimi3, Muhammet Karaman4, İlhami Gulçin5.
Abstract
A series of substituted pyrazole compounds (1-8 and 9a, b) were synthesized and their structure was characterized by IR, NMR, and Mass analysis. These obtained novel pyrazole derivatives (1-8 and 9a, b) were emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 1.03 ± 0.23-22.65 ± 5.36 µM for hCA I, 1.82 ± 0.30-27.94 ± 4.74 µM for hCA II, and 48.94 ± 9.63-116.05 ± 14.95 µM for AChE, respectively. Docking studies were performed for the most active compounds, 2 and 5, and binding mode between the compounds and the receptors were determined.Entities:
Keywords: Acetylcholinesterase; Carbonic anhydrase; Enzyme inhibition; Substituted pyrazole
Year: 2019 PMID: 30769267 DOI: 10.1016/j.bioorg.2019.02.013
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275