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oai:ojs.www.eurjchem.com:article/878 2013-12-31T06:16:57Z eurjchem:ART driver

Synthesis, characterization and in vitro biological evaluation of some new diarylsulfonylurea-chalcone hybrids as potential 5-lipoxygenase inhibitors Bugata, Bharat Kumar Dowluru, Satya Venkata Gopala Krishna Kaladhar Avupati, Vasudeva Rao Gavalapu, Venkateswara Rao Nori, Divakara Laxman Somayajulu Barla, Sreenu Chalcone 5-Lipoxygenase Diarylsulfonylurea Abietic acid (LI01020) Claisen-Schmidt condensation Diarylsulfonylurea-chalcone hybrid 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. Atlanta Publishing House LLC 2013-12-31 info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion application/pdf https://www.eurjchem.com/index.php/eurjchem/article/view/878 10.5155/eurjchem.4.4.396-401.878 European Journal of Chemistry; Vol. 4 No. 4 (2013): December 2013; 396-401 2153-2257 2153-2249 eng https://www.eurjchem.com/index.php/eurjchem/article/view/878/PDF