Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS was written by Saha, Ashis K.;Yu, Xiang;Lin, Jian;Lobera, Mercedes;Sharadendu, Anurag;Chereku, Srinivas;Schutz, Nili;Segal, Dalia;Marantz, Yael;McCauley, Dilara;Middleton, Scot;Siu, Jerry;Burli, Roland W.;Buys, Janet;Horner, Michelle;Salyers, Kevin;Schrag, Michael;Vargas, Hugo M.;Xu, Yang;McElvain, Michele;Xu, Han. And the article was included in ACS Medicinal Chemistry Letters in 2011.Formula: C8H6O2 This article mentions the following:
Novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity were prepared 1-{[4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl]methyl}azetidine-3-carboxylic acid is a potent S1P1 agonist with >1000× selectivity over S1P3. It demonstrated a good in vitro ADME profile and excellent oral bioavailability across species. Dosed orally at 0.3 mg/kg, I significantly reduced blood lymphocyte counts 24 h postdose and demonstrated efficacy in a mouse EAE model of relapsing MS. In the experiment, the researchers used many compounds, for example, Benzofuran-5-ol (cas: 13196-10-6Formula: C8H6O2).
Benzofuran-5-ol (cas: 13196-10-6) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Formula: C8H6O2
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem