Bis-Schiff bases 1-27 have been synthesized and their in vitro antiglycation potential has been evaluated. Compounds 21 (IC(50)=243.95+/-4.59microM), 20 (IC(50)=257.61+/-5.63microM), and 7 (IC(50)=291.14+/-2.53microM) showed an excellent antiglycation activity better than the standard (rutin, IC(50)=294.46+/-1.50microM). This study has identified a series of potential molecules as antiglycation agents. A structure-activity relationship has been studied, and all the compounds were characterized by spectroscopic techniques.