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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
VOLUME: 10
ISSUE: 8
DOI: 10.2174/1573406410666140331230953      Price:  $58









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

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Author(s): Sanaullah Abbasi, Salma Mirza, Saima Rasheed, Shafqat Hussain, Jalaluddin A.J. Khan, Khalid Mohammed Khan, Shahnaz Perveen and Muhammad Iqbal Choudhary
Pages 824-835 (12)
Abstract:
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.
Affiliation:
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.