Some new thiazolyl thiazolidinedione derivatives as a1dose reductase inhibitors

Bozdag-Duendar O., Evcimen N. D., Ceylan-Uenluesoy M., Ertan R., Sarikaya M.

MEDICINAL CHEMISTRY RESEARCH, cilt.16, sa.1, ss.39-47, 2007 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 16 Sayı: 1
  • Basım Tarihi: 2007
  • Doi Numarası: 10.1007/s00044-007-9008-9
  • Dergi Adı: MEDICINAL CHEMISTRY RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.39-47
  • Anahtar Kelimeler: synthesis, thiazole derivatives, 2,4-Thiazolidinediones aldose reductase inhibition, ALDOSE REDUCTASE, AGENT CS-045, PREVENTION, GLUCOSE
  • Ankara Üniversitesi Adresli: Evet

Özet

In diabetes, increased flux through the polyol pathway has been implicated in the development of diabetic complications such as cataract, retinopathy, neuropathy, and nephropathy. Aldose reductase (AR) appears to be the key factor in the reduction of glucose to sorbitol. Aldose reductase inhibitors have been found to prevent sorbitol accumulation in tissues. A series of thiazolyl-2,4-thiazolidinediones was prepared by Knoevenagel reaction of substituted benzyl-2,4-thiazolidinediones with chlorothiazolecarbaldehydes and were evaluated for their ability to inhibit rat kidney AR by an in vitro spectrophotometric assay. Results showed that compounds containing piperidine at the C-2 position of thiazole ring showed better inhibitory activity than thiazole compounds having 4-chlorobenzylsulfanyl at the same position.