A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activities of these compounds.
|Data di pubblicazione:||2007|
|Titolo:||Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system|
|Autori:||HARRAK Y; ROSELL G; DAIDONE G; PLESCIA S; SCHILLACI D; PUJOL MD|
|Tipologia:||Articolo su rivista|
|Citazione:||HARRAK Y, ROSELL G, DAIDONE G, PLESCIA S, SCHILLACI D, & PUJOL MD (2007). Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system. BIOORGANIC & MEDICINAL CHEMISTRY, 15, 4876-4890.|
|Digital Object Identifier (DOI):||10.1016/j.bmc.2007.04.050|
|Appare nelle tipologie:||01 - Articolo su rivista|