Synthesis and biological evaluation of a novel series of bis-salicylaldehydes as mushroom tyrosinase inhibitors

Giovanna Delogu; Gianni Podda; Marcella Corda; Maria Benedetta Fadda; Antonella Fais; Benedetta Era

doi:10.1016/j.bmcl.2010.08.018

Synthesis and biological evaluation of a novel series of bis-salicylaldehydes as mushroom tyrosinase inhibitors

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6138-40. doi: 10.1016/j.bmcl.2010.08.018. Epub 2010 Aug 10.

Authors

Giovanna Delogu¹, Gianni Podda, Marcella Corda, Maria Benedetta Fadda, Antonella Fais, Benedetta Era

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Cagliari, Cagliari, CA, Italy. delogug@unica.it

PMID: 20813526
DOI: 10.1016/j.bmcl.2010.08.018

Abstract

A series of novel bis-salicylaldehydes were synthesised and evaluated as tyrosinase inhibitors using a tyrosinase-dependent L-DOPA oxidation assay. The bis-salicylaldehydes exhibited greater inhibitory activity than salicylaldehyde. Our data suggests that these novel compounds may serve as a structural template for the design and development of novel tyrosinase inhibitors.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Agaricales / enzymology*
Aldehydes / chemical synthesis
Aldehydes / chemistry*
Aldehydes / pharmacology*
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Inhibitory Concentration 50
Monophenol Monooxygenase / antagonists & inhibitors*
Monophenol Monooxygenase / metabolism
Oxidation-Reduction

Substances

Aldehydes
Enzyme Inhibitors
salicylaldehyde
Monophenol Monooxygenase