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

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

Volume: 10 Issue: 8

Author(s): Sanaullah Abbasi, Salma Mirza, Saima Rasheed, Shafqat Hussain, Jalaluddin A.J. Khan, Khalid Mohammed Khan, Shahnaz Perveen and Muhammad Iqbal Choudhary

Affiliation:

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

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.

Cite this article as:

Abbasi Sanaullah, Mirza Salma, Rasheed Saima, Hussain Shafqat, Khan A.J. Jalaluddin, Khan Mohammed Khalid, Perveen Shahnaz and Choudhary Iqbal Muhammad, Benzothiazole Derivatives: Novel Inhibitors of Methylglyoxal Mediated Glycation of Proteins In Vitro, Medicinal Chemistry 2014; 10 (8) . https://dx.doi.org/10.2174/1573406410666140331230953