Synthesis, characterization, molecular docking and biological activities of novel pyrazoline derivatives

  • Turkan, F.
  • Çetin, A.
  • Taslimi, P.
  • Karaman H.S.
  • Gulçin İ.
Publication date
January 2019
Publisher
Wiley-VCH Verlag
Journal
Archiv der Pharmazie

Abstract

PubMed ID: 31125504In 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 Ki 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 t...

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