Sunday, December 16, 2018

Aromatic Aldehydes and #CarboxylicAcids as inhibitors for Sickle #HemoglobinPolymerization by Ahmed S Mehanna in BJSTR

Abstract

The reported inhibitory effects of the natural products vanillin and 5-hydroxymethylfurfural prompted us to assess the anti-polymerization activities of several structurally related aromatic #aldehydes and #carboxylicacids. In addition to vanillin and #5-hydroxymethylfurfural, eleven more structurally related aromatic aldehydes and carboxylic acids including 2,4-dihydroxy benzaldehyde, furfural, 3-furfural, 5-methylfurfural, vanillic acid, 2-hydroxy-3-methoxy-benzoic acid, homovanillic acid, mandelic acid, 4-hydroxy-3-methoxy-mandelic acid, 4-bromo-mandelic acid and4-trifluromethyl-mandemic acid are evaluated for activity using our newly reported high throughput kinetic assay designed to study sickle cell hemoglobin polymerization kinetics. Several of the tested compounds exhibited promising anti-polymerization activities, comparable to that of vanillin and 5-hydroxymethylfurfural, including #homovanillicacid, #mandelicacid, 3-hydroxy-3-methoxymandelic acid, and 3-furfural. The structure activity relationship of all tested compounds is included.

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