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. 2021 Sep:114:105128.
doi: 10.1016/j.bioorg.2021.105128. Epub 2021 Jun 29.

Microwave-assisted rapid synthesis of spirooxindole-pyrrolizidine analogues and their activity as anti-amyloidogenic agents

Nilamuni H de Silva  1 , Suneela Pyreddy  1 , Ewan W Blanch  1 , Helmut M Hügel  2 , Subashani Maniam  3
Affiliations

Microwave-assisted rapid synthesis of spirooxindole-pyrrolizidine analogues and their activity as anti-amyloidogenic agents

Nilamuni H de Silva et al. Bioorg Chem. 2021 Sep.

Abstract

A library of Sox-pyrrolizidines was rapidly prepared by microwave-assisted, one-pot, three-component, 1,3-dipolar cycloaddition of azomethine ylides from l-proline and isatin, with various β-nitrostyrenes. Nitro-Sox compounds, 4b, 4d and 4e inhibit HEWL amyloid fibril formation by ThT studies with percentages of fluorescence intensity of 55.4, 42.9 and 40.3%, respectively. Further studies with MTT assay, Raman spectroscopy, TEM and molecular docking supported these promising candidates for activity against amyloid misfolding, a phenomenon leading to Alzheimer's disease pathology.

Keywords: Alzheimer’s disease; Amyloid beta; Fluorescence inhibition; Neuroprotection; Protein misfolding; Spicocyclics.

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