Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

Back

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

Author(s): 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.

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

Graphical Abstract:


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.

Reprint ePrint Rights & PermissionsPrintExport

Article Details

VOLUME: 10
ISSUE: 8
Page: [824 - 835]
Pages: 12
DOI: 10.2174/1573406410666140331230953