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Article Dans Une Revue Bioorganic Chemistry Année : 2020

Synthesis, docking and evaluation of in vitro anti-inflammatory activity of novel morpholine capped β-lactam derivatives

Résumé

This study reports the synthesis and biological investigation of three series of novel β-lactams bearing a morpholine substituent of the nitrogen center. These products were synthesized via Staudinger's [2+2]-ketene-imine cycloaddition reaction. The cycloadducts were fully characterized by spectral data, including 1 H-NMR, 13 C-NMR, IR, mass spectroscopy and elemental analyses, and then evaluated for anti-inflammatory activity. A number of the derivatives demonstrated higher therapeutic ratios than dexamethasone and corticosteroid medication. In silico molecular docking experiments showed a good correlation between the experimental activity and the calculated binding affinity to human inducible nitric oxide synthase, the enzymatic target for the anti-inflammatory response.
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Dates et versions

hal-03085012 , version 1 (12-01-2021)

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Roghayeh Heiran, Saghi Sepehri, Aliasghar Jarrahpour, Carole Digiorgio, Hana Douafer, et al.. Synthesis, docking and evaluation of in vitro anti-inflammatory activity of novel morpholine capped β-lactam derivatives. Bioorganic Chemistry, 2020, 102, pp.104091. ⟨10.1016/j.bioorg.2020.104091⟩. ⟨hal-03085012⟩
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