Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones


Bozdak-Dundar O., Evranos B., Das-Evcimen N., Sarikaya M., Ertan R.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.43, sa.11, ss.2412-2417, 2008 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 43 Sayı: 11
  • Basım Tarihi: 2008
  • Doi Numarası: 10.1016/j.ejmech.2008.01.004
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.2412-2417
  • Anahtar Kelimeler: Chromone derivatives, 2,4-Thiazolidinediones, Chromonyl-2,4-thiazolidinediones, Aldose reductase, Aldose reductase inhibition, Synthesis, DIABETIC COMPLICATIONS, ALDEHYDE REDUCTASES, AGENT CS-045, DERIVATIVES, CONSTITUENTS, FLAVONOIDS, PLANTS, NIDDM, ACIDS, RATS
  • Ankara Üniversitesi Adresli: Evet

Özet

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 chromonl-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 la-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). (C) 2008 Elsevier Masson SAS. All rights reserved.