Benzothiazole Derivatives: Novel Inhibitors of Methylglyoxal Mediated Glycation of Proteins In Vitro

This manuscript describes the protein anti-glycation activity of thirty-three (33) benzothiazoles, out of which twenty-seven were the newly synthesized benzothiazoles. Compound 1 (IC 50 = 187 ± 2.6 µM) was found to be the most active, while compounds 2 (IC 50 = 219 ± 3.6 µM), 3 (IC 50 = 224 ± 1.9 µM), 4 (IC 50 = 223 ± 3.3 µM), 5 (IC 50 = 238 ± 2.2 µM), 7 (IC 50 = 266 ± 5.4 µM), 17 (IC 50 = 226 ± 1.6 µM) and 18 (IC 50 = 274 ± 2.4 µM) were significantly active, when compared with the standard rutin (IC 50 = 294 ± 1.5 µM). This study identified potential inhibitors of methylglyoxal mediated glycation of proteins, which is the pathophysiology of late diabetic complications.