Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.

Article Details

Citation

Copy to clipboard

Hansen FK, Khankischpur M, Tolaymat I, Mesaros R, Dannhardt G, Geffken D

Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):5031-4. doi: 10.1016/j.bmcl.2012.06.012. Epub 2012 Jun 13.

PubMed ID

22749420 [ View in PubMed

]

Abstract

A series of 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives has been prepared and subsequently evaluated with regards to the inhibition of 5-LOX/COX. Structure optimization furnished derivatives with promising in vitro activity as dual 5-LOX/COX inhibitors with submicromolar IC(50) values for inhibition of 5-LOX and COX-1, respectively.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Celecoxib	Prostaglandin G/H synthase 2	IC 50 (nM)	140	N/A	N/A	Details
Indomethacin	Prostaglandin G/H synthase 2	IC 50 (nM)	500	N/A	N/A	Details