A series of metronidazole ester derivatives 1-34 has been synthesized with the aim of developing new leads with antiglycation activity. The in vitro evaluation of antiglycation potential of 1-34 showed that the ester derivatives 28, 16, and 3 have IC(50) values 218.97 ± 2.5, 245.3 ± 5.1, and 278.6 ± 0.8 µM, respectively, comparable to the standard agent, rutin (IC(50) = 294.5 ± 1.50 µM). The study identifies a new class of potent antiglycation agents. A structure-activity relationship has also been evaluated. All the compounds were characterized by using spectroscopic techniques, including (1)H NMR, IR, and EI-MS.