Synthesis, characterization and in vitro biological evaluation of some new diarylsulfonylurea-chalcone hybrids as potential 5-lipoxygenase inhibitors
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Accepted 2013-08-06
Published 2013-12-31
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Abstract
A series of some new diarylsulfonylurea-chalcone hybrids (4a-4y) have been synthesized via Claisen-Schmidt condensation reaction by treating 1-(3-acetylphenyl)-3-tosylurea with various aromatic/heteroaromatic aldehydes in the presence of alkali and characterized by FT-IR, 1H NMR, 13C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro 5-Lipoxygenase inhibitory activity using potato 5-lipoxygenase enzyme. Among the tested compounds 4r and 4o exhibited significant inhibitory activity at IC50 values 7.88±0.14 and 11.77±0.21 µg/mL, respectively. This level of activity was found comparable to that of the reference drug Abietic acid (LI01020) with IC50 value 4.34±0.37 µg/mL and it could be a remarkable starting point to develop new lead molecules.
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Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
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