Small synthetic molecules with antiglycation activity. Structure–activity relationship

Abstract

The accumulation of advanced glycation end products (AGEs) is currently considered as one of the key factors in aging processes, the pathogenesis of late complications of diabetes mellitus, cancer and neurodegenerative diseases. This review is devoted to small synthetic molecules with antiglycation activity, i.e., compounds with the ability to inhibit AGE formation. Molecules with antiglycation activity in the low micromolar range (<10 μM), primarily fused heterocyclic systems containing oxygen or nitrogen as heteroatoms and (thio)ureas, have been discovered to date. The known scaffolds with antiglycation activity are analyzed, structural modifications to enhance antiglycation abilities are highlighted and the structure–activity relationships are discussed. The bibliography includes 125 references.

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“…Based on the structure-activity relationship (SAR) study, the presence of a hydroxyl/nitro group and halogen atoms in the phenol ring enhances antiglycation activity; on the other hand, alkyl, trifluoromethyl, and bulky groups reduce the activity. Likewise, the activity is lost by phenyl group replacement by hetaryl or nonaromatic groups or if a blend of various scaffoldings is present in a single molecule [50]. Additionally, methoxy groups decrease the inhibition [51], as observed for TMA.…”