Benzothiazole derivatives: novel inhibitors of methylglyoxal mediated glycation of proteins in vitro.
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.
Sanaullah
S
Abbasi
Salma
S
Mirza
Saima
S
Rasheed
Shafqat
S
Hussain
Jalaluddin A J
JA
Khan
Khalid Mohammed
KM
Khan
Shahnaz
S
Perveen
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. khalid.khan@iccs.edu.
Muhammad Iqbal
MI
Choudhary
D016475:3T3 Cells; D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D002645:Chickens; D017127:Glycation End Products, Advanced / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006031:Glycosylation / Q000187:drug effects; D051379:Mice; D009113:Muramidase / Q000037:antagonists & inhibitors / Q000737:chemistry; D011765:Pyruvaldehyde / Q000737:chemistry*; D012431:Rutin / Q000494:pharmacology; D012710:Serum Albumin, Bovine / Q000037:antagonists & inhibitors / Q000737:chemistry; D013329:Structure-Activity Relationship
D052160:Benzothiazoles; D017127:Glycation End Products, Advanced; D012710:Serum Albumin, Bovine; D012431:Rutin; D011765:Pyruvaldehyde; D009113:Muramidase