Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as 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.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt. ayoussef65@yahoo.com
Amal M
AM
Youssef
M Sydney
MS
White
Erika B
EB
Villanueva
Ibrahim M
IM
El-Ashmawy
Andis
A
Klegeris
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D051545:Cyclooxygenase 1 / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000378:metabolism; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D006099:Granuloma / Q000139:chemically induced / Q000188:drug therapy; D018922:HL-60 Cells; D006801:Humans; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051381:Rats; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use
D000893:Anti-Inflammatory Agents; D018696:Neuroprotective Agents; D045162:Thiazolidinediones; C089946:2,4-thiazolidinedione; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2