Benzothiazole Derivatives: Novel Inhibitors of Methylglyoxal Mediated Glycation of Proteins In Vitro
Sanaullah Abbasi, Salma Mirza, Saima Rasheed, Shafqat Hussain, Jalaluddin A.J. Khan, Khalid Mohammed Khan, Shahnaz Perveen and Muhammad Iqbal Choudhary
Affiliation: H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
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 (IC50= 187 ± 2.6 µM) was found to be the most
active, while compounds 2 (IC50= 219 ± 3.6 µM), 3 (IC50= 224 ± 1.9 µM), 4 (IC50= 223 ± 3.3 µM), 5 (IC50= 238 ± 2.2 µM), 7 (IC50= 266 ± 5.4 µM), 17 (IC50= 226 ± 1.6 µM) and 18 (IC50= 274 ± 2.4 µM) were significantly active, when
compared with the standard rutin (IC50= 294 ± 1.5 µM). This study identified potential inhibitors of methylglyoxal mediated
glycation of proteins, which is the pathophysiology of late diabetic complications.
Keywords: Diabetes, Maillard reaction, Benzothiazoles, Advanced glycation endproducts (AGEs), Benzothiazoles, Protein
glycation inhibition, Diabetic complications.
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