2930-02-1Relevant articles and documents
Regioselective ring-opening of epoxides by carbazole: A direct preparation of novel N-(β-hydroxyalkyl)carbazoles
Soltani Rad, Mohammad Navid,Behrouz, Somayeh,Ahrari, Samira
, p. 137 - 140 (2016/04/20)
The influence of various parameters including solvent, base and temperature on the reaction between carbazole and epoxides was studied This led to the development of a regioselective ring-opening of epoxides by the potassium salt of carbazole in DMSO at 100 °C which is a straightforward way to prepare new N-(β-hydroxyalkyl)carbazoles in good to excellent yields. Fifteen new compounds are described.
Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization
Tasler, Stefan,Baumgartner, Roland,Ammendola, Astrid,Schachtner, Josef,Wieber, Tanja,Blisse, Marcus,Rath, Sandra,Zaja, Mirko,Klahn, Philipp,Quotschalla, Udo,Ney, Peter
scheme or table, p. 6108 - 6115 (2010/11/19)
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC50 = 20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.