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

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Harrak Y, Rosell G, Daidone G, Plescia S, Schillaci D, Pujol MD

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

Bioorg Med Chem. 2007 Jul 15;15(14):4876-90. Epub 2007 May 3.

PubMed ID

17517512 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Ibuprofen	Prostaglandin G/H synthase 1	IC 50 (nM)	6900	N/A	N/A	Details
Ibuprofen	Prostaglandin G/H synthase 2	IC 50 (nM)	6200	N/A	N/A	Details