Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones.
As it is known that still, there were no any confident ARIs on the market and they have several side effects, we need to approve new ARIs to reduce diabetic complications especially which have effect on the cataract formation. In this study, a new series of chromonyl-2,4-thiazolidinediones (Ia-e, IIa-e, IIIa-e) were prepared by Knoevenagel reaction with substituted 3-formylchromones (3a-e) and unsubstituted (1) or substituted 2,4-thiazolidinedione (2). The synthesized compounds were tested for their ability to inhibit rat kidney AR by an in vitro spectrophotometric assay. Compound IIIe showed the highest inhibitory activity (82.43+/-0.76%). Compounds Ia-e and IIIa-d also showed significant inhibitory activity (42.40+/-5.78, 52.71+/-3.31, 49.69+/-1.55, 50.80+/-3.62, 46.70+/-2.33, 49.44+/-4.53, 61.17+/-4.74, 68.58+/-2.05, 77.28+/-0.26%, respectively).
Bozdağ-Dündar
Oya
O
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey. bozdag@pharmacy.ankara.edu.tr
Evranos
Begüm
B
Daş-Evcimen
Net
N
Sarikaya
Mutlu
M
Ertan
Rahmiye
R
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008297:Male; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D045162:Thiazolidinediones; C089946:2,4-thiazolidinedione; D000449:Aldehyde Reductase