33851-23-9Relevant academic research and scientific papers
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives
Hansen, Finn K.,Khankischpur, Mehdi,Tolaymat, Ibrahim,Mesaros, Renata,Dannhardt, Gerd,Geffken, Detlef
scheme or table, p. 5031 - 5034 (2012/08/28)
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 IC50 values for inhibition of 5-LOX and COX-1, respectively.
Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors
Moretto,Kirincich,Xu,Smith,Wan,Wilson,Follows,Binnun,Joseph-McCarthy,Foreman,Erbe,Zhang,Tam,Tam,Lee
, p. 2162 - 2177 (2007/10/03)
A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations. The potency of this lead compound has been improved significantly by medicinal chemistry guided by X-ray crystallo
Inhibitors of protein tyrosine phosphatase 1B
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Page/Page column 46-47, (2008/06/13)
Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
