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

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)

Volume 10, 8 Issues, 2014

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Medicinal Chemistry

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Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge

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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


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


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

Keywords: Diabetes, Maillard reaction, Benzothiazoles, Advanced glycation endproducts (AGEs), Benzothiazoles, Protein glycation inhibition, Diabetic complications

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Article Details

Volume: 10
First Page: 1
Last Page: 12
Page Count: 12
DOI: 10.2174/1573406410666140331230953

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