6533b86dfe1ef96bd12ca194

RESEARCH PRODUCT

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

Renata MesarosIbrahim TolaymatFinn K. HansenFinn K. HansenDetlef GeffkenGerd DannhardtMehdi Khankischpur

subject

StereochemistryCarboxylic acidClinical BiochemistryCarboxylic AcidsPharmaceutical ScienceThiophenesInhibitory postsynaptic potentialBiochemistryStructure-Activity Relationshipchemistry.chemical_compoundDrug DiscoveryThiopheneCyclooxygenase InhibitorsLipoxygenase InhibitorsMolecular Biologychemistry.chemical_classificationArachidonate 5-Lipoxygenaseintegumentary systemOrganic Chemistryfood and beveragesBenzothiopheneIn vitrochemistryCyclooxygenase 1Molecular MedicineLicofeloneProtein Binding

description

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.

yearjournalcountryeditionlanguage
2012-05-04Bioorganic & Medicinal Chemistry Letters
https://doi.org/10.1016/j.bmcl.2012.06.012