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 M), primarily fused heterocyclic systems containing oxygen or nitrogen as heteroatoms and (thio)ureas, were discovered. The known scaffolds with antiglycation activity are analyzed, structural modifications to enhance antiglycation abilities are highlighted and the structure--activity relationships are discussed. Bibliography --- 125 references.