Details

Autor(en) / Beteiligte

• Youssef, Amal M.
• Sydney White, M.
• Villanueva, Erika B.
• El-Ashmawy, Ibrahim M.
• Klegeris, Andis

Titel

Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents

Ist Teil von

• Bioorganic & medicinal chemistry, 2010-03, Vol.18 (5), p.2019-2028

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• A number of in vitro and in vivo assays were used to identify four novel pyrazolyl-2,4-thiazolidinediones ( 5a– c, 7b) as potential anti-inflammatory and neuroprotective agents. Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds were further studied in vivo by using the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays. We identified four novel compounds that showed protective effects in vitro at non-toxic concentrations, and were also effective in the animal models of acute and sub-acute inflammation.