Abstract
Starting with salicylaldehyde, compounds (I) [1-(2-hydroxybenzyl)piperidinium chloride] and (II) [4-carbamoyl-1-(2-hydroxybenzyl)piperidinium chloride] were prepared via multi step synthesis. The synthesized compounds were evaluated in vivo for their anti-inflammatory, analgesic, and anti-pyretic activities. Both compounds showed significant pharmacological profile when compared with reference standard, aspirin. In an attempt to understand the ligand–protein interaction in terms of the binding affinity, the synthetic molecule II was subjected to docking analysis using AutoDock which showed better binding modes with the active sites of COX’s enzymes.
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Acknowledgments
The authors gratefully acknowledge the Higher Education Commission of Pakistan for financial support for research. The authors sincerely thank and acknowledge PCSIR laboratories, Peshawar, Pakistan and Punjab Drug House (PDH), Lahore for providing some reagents.
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Ullah, N., Ul Islam, N., Ali, G. et al. Bioisosteric synthesis of nitrogen containing derivatives of salicyl alcohol, their in vivo pharmacological studies with molecular modeling. Med Chem Res 22, 4677–4684 (2013). https://doi.org/10.1007/s00044-013-0473-z
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DOI: https://doi.org/10.1007/s00044-013-0473-z