European Journal of Chemistry

Synthesis, characterization and in vitro biological evaluation of some new diarylsulfonylurea-chalcone hybrids as potential 5-lipoxygenase inhibitors

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Published: Dec 31, 2013
DOI: https://doi.org/10.5155/eurjchem.4.4.396-401.878
Keywords:
Chalcone, 5-Lipoxygenase, Diarylsulfonylurea, Abietic acid (LI01020), Claisen-Schmidt condensation, Diarylsulfonylurea-chalcone hybrid
Section
Research Article
Issue
Vol. 4 No. 4 (2013): December 2013
Dates
Received 2013-07-15
Accepted 2013-08-06
Published 2013-12-31


Main Article Content

Bharat Kumar Bugata
Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Satya Venkata Gopala Krishna Kaladhar Dowluru
Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Vasudeva Rao Avupati
Pharmaceutical Chemistry Division, Andhra University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530003, Andhra Pradesh, India
Venkateswara Rao Gavalapu
Pharmaceutical Chemistry Division, Andhra University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530003, Andhra Pradesh, India
Divakara Laxman Somayajulu Nori
Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Sreenu Barla
Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

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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Bugata, B. K.; Dowluru, S. V. G. K. K.; Avupati, V. R.; Gavalapu, V. R.; Nori, D. L. S.; Barla, S. Synthesis, Characterization and in Vitro Biological Evaluation of Some New Diarylsulfonylurea-Chalcone Hybrids As Potential 5-Lipoxygenase Inhibitors. Eur. J. Chem. 2013, 4, 396-401.

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Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
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