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Synthesis, characterization, lipoxygenase inhibitory activity and in silico molecular docking of biaryl bis(benzenesulfonamide) and indol-3-yl-hydrazide derivatives

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Abstract

In this paper, we have screened a library of two different series of compounds to identify potent lipoxygenase (LOX) inhibitors. A number of new biphenyl bis(benzenesulfonamides) 23, indol-3-yl-benzenesulfonyl and acetohydrazides 45 and indol-3-yl-hydrazinecarboxylate 6 were synthesized and evaluated in vitro for LOX inhibitory activity. Compounds biphenyl bis(benzenesulfonamide) 2a and indol-3-yl-benzenesulfonylhydrazide 4e presented the best anti-LOX activity within these series with IC50 values 96.31 ± 0.18 and 81.21 ± 2.14 μM, respectively. The results were confirmed with docking studies.

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Acknowledgments

We acknowledge the Higher Education Commission and Ministry of Science and Technology, Pakistan, for financial support.

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The authors have declared no conflict of interest.

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Mutahir, S., Yar, M., Khan, M.A. et al. Synthesis, characterization, lipoxygenase inhibitory activity and in silico molecular docking of biaryl bis(benzenesulfonamide) and indol-3-yl-hydrazide derivatives. J IRAN CHEM SOC 12, 1123–1130 (2015). https://doi.org/10.1007/s13738-014-0573-9

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