Synthesis and biological activity of some new flavonyl-2,4-thiazolidinediones.
A new series of flavonyl-2,4-thiazolidinediones (Va-c, VIa-c) was prepared by Knoevenagel reaction. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR) and for their insulinotropic activities in INS-1 cells. Compound Vb was able to increase insulin release in the presence of 5.6mmol/l glucose. Compounds VIa-c displayed moderate to high AR inhibitory activity levels. Particularly, compound VIa showed the highest AR inhibitory activity (86.57%).
Bozdağ-Dündar
Oya
O
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandoğan, Ankara, Turkey. bozdag@pharmacy.ankara.edu.tr
Verspohl
Eugen J
EJ
Daş-Evcimen
Net
N
Kaup
Rebecca M
RM
Bauer
Katrin
K
Sarikaya
Mutlu
M
Evranos
Begüm
B
Ertan
Rahmiye
R
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors; D000818:Animals; D002460:Cell Line; D005947:Glucose / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007668:Kidney / Q000201:enzymology; D008297:Male; D051379:Mice; D051381:Rats; D045162:Thiazolidinediones / Q000737:chemistry* / Q000494:pharmacology*
D007004:Hypoglycemic Agents; D007328:Insulin; D045162:Thiazolidinediones; D000449:Aldehyde Reductase; D005947:Glucose