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.

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(14), 4876-4890 [10.1016/j.bmc.2007.04.050].

Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system

DAIDONE, Giuseppe;PLESCIA, Salvatore;SCHILLACI, Domenico;
2007-01-01

Abstract

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.
2007
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(14), 4876-4890 [10.1016/j.bmc.2007.04.050].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/9400
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