Title: Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities.
Authors: Hendriks, Christine M M; Penning, Trevor M; Zang, Tianzhu; Wiemuth, Dominik; Gründer, Stefan; Sanhueza, Italo A; Schoenebeck, Franziska; Bolm, Carsten
Published In Bioorg Med Chem Lett, (2015 Oct 15)
Abstract: Pentafluorosulfanyl-containing analogs of flufenamic acid have been synthesized in high yields. Computationally, pKa, LogP and LogD values have been determined. Initial bioactivity studies reveal effects as ion channel modulators and inhibitory activities on aldo-keto reductase 1C3 (AKR1C3) as well as COX-1 and COX-2.
PubMed ID: 26372652
MeSH Terms: 3-Hydroxysteroid Dehydrogenases/antagonists & inhibitors*; 3-Hydroxysteroid Dehydrogenases/metabolism; Aldo-Keto Reductase Family 1 Member C3; Cyclooxygenase 1/metabolism*; Cyclooxygenase 2/metabolism*; Dose-Response Relationship, Drug; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology*; Flufenamic Acid/chemical synthesis; Flufenamic Acid/chemistry; Flufenamic Acid/pharmacology*; Humans; Hydroxyprostaglandin Dehydrogenases/antagonists & inhibitors*; Hydroxyprostaglandin Dehydrogenases/metabolism; Molecular Structure; Structure-Activity Relationship; Sulfhydryl Compounds/chemistry*