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

Abstract

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.

• Authors: Amal M Youssef, M Sydney White, Erika B Villanueva, Ibrahim M El-Ashmawy, Andis Klegeris
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 18 Issue 5 Pg. 2019-28 (Mar 01 2010) ISSN: 1464-3391 [Electronic] England
• PMID: 20138770 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Inflammatory Agents
• Neuroprotective Agents
• Thiazolidinediones
• 2,4-thiazolidinedione
• Cyclooxygenase 1
• Cyclooxygenase 2

Topics

• Animals
• Anti-Inflammatory Agents (chemical synthesis, chemistry, therapeutic use)
• Cell Line, Tumor
• Cyclooxygenase 1 (metabolism)
• Cyclooxygenase 2 (metabolism)
• Edema (chemically induced, drug therapy)
• Granuloma (chemically induced, drug therapy)
• HL-60 Cells
• Humans
• Neuroprotective Agents (chemical synthesis, chemistry, therapeutic use)
• Rats
• Thiazolidinediones (chemical synthesis, chemistry, therapeutic use)