Design, synthesis and antiinflammatory activity of novel phthalimide derivatives, structurally related to thalidomide.
As part of an ongoing effort to develop new thalidomide analogues as antiinflammatory lead-candidates, this paper describes the synthesis and antiinflammatory activity of novel N-phenyl-phthalimide functionalized derivatives (4a-d, 5a,b, 6a,b). The target compounds were assayed in an acute lung inflammatory model and all compounds were able to inhibit TNF-alpha production and subsequent neutrophil recruitment in the LPS-acute lung inflammatory model.
Machado
Alexandre Légora
AL
Instituto Bioquímica Médica, Universidade Federal do Rio de Janeiro, Brazil.
Lima
Lídia Moreira
LM
Araújo
João Xavier
JX
Fraga
Carlos Alberto M
CA
Koatz
Vera Lúcia Gonçalves
VL
Barreiro
Eliezer J
EJ
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002633:Chemotaxis / Q000187:drug effects; D015195:Drug Design; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D008070:Lipopolysaccharides / Q000494:pharmacology; D008171:Lung Diseases / Q000139:chemically induced / Q000188:drug therapy; D051379:Mice; D009504:Neutrophils / Q000187:drug effects; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013792:Thalidomide / Q000737:chemistry; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors
D000893:Anti-Inflammatory Agents; D008070:Lipopolysaccharides; D010797:Phthalimides; D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide