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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
Epub Full Text Article
DOI: 10.2174/1573406410666140331230953      Price:  $95

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

Author(s): Sanaullah Abbasia, Salma Mirzab, Saima Rasheedb, Shafqat Hussainb, Jalaluddin A. J. Khana, Khalid Mohammed Khanb, Shahnaz Perveenc, M. Iqbal Choudharya and b
This manuscript describes the protein anti-glycation activity of thirty-three (33) benzothiazoles, out of which twenty-seven were 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 ± 3.6 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
Diabetes, Maillard reaction, Benzothiazoles, Advanced glycation endproducts (AGEs), Benzothiazoles, Protein glycation inhibition, Diabetic complications

aDepartment of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah-22254, Saudi Arabia

bH. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan

cPCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi-75280, Pakistan