Journal
ARCHIV DER PHARMAZIE
Volume 352, Issue 6, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201800359
Keywords
acetylcholinesterase; enzyme inhibition; human carbonic anhydrase; in silico study; induced fit docking; pyrazoline
Funding
- Scientific Research Fund of Igdir University [2018-SBE-A01]
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In this study, synthesis of ethyl 2-((4-bromophenyl)diazenyl)-3-oxo-phenylpropanoate 1 was carried out and a series of new 3H-pyrazol-3-ones (P1-7) were synthesized from 1 as well as various hydrazines. The obtained yields of the synthesized compounds were moderate (40-70%) and these compounds were confirmed by spectral data. These novel pyrazoline derivatives were effective inhibitor compounds of the human carbonic anhydrase I and II isozymes (hCAs I and II) and of the acetylcholinesterase (AChE) enzyme, with K-i values in the range of 17.4-40.7 nM for hCA I, 16.1-55.2 nM for hCA II, and 48.2-84.1 nM for AChE. In silico studies were performed on the compounds inhibiting hCA I, hCA II, and AChE receptors. On the basis of the findings, the inhibition profile of the new pyrazoline compounds at the receptors was determined.
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