Burkholder, Timothy P.; Kudlacz, Elizabeth M.; Maynard, George D.; Liu, Xiao-Gao; Le, Tieu-Binh; Webster, Mark E.; Horgan, Stephen W.; Wenstrup, David L.; Freund, David W.; Boyer, Fred; Bratton, Larry; Gross, Raymond S.; Knippenberg, Robert W.; Logan, Deborah E.; Jones, Bryan K.; Chen, Teng-Man; Geary, Julie L.; Correll, Melinda A.; Poole, J. Chuck; Mandagere, Arun K.; Thompson, Thomas N.; Hwang, Kin-Kai published the artcile< Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists>, Category: nitriles-buliding-blocks, the main research area is pyrrolidine preparation neurokinin receptor antagonist; structure activity pyrrolidine neurokinin receptor antagonist.
The authors recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here, the authors report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212, I (Ar1 = 3-ClC6H4, 4-FC6H4, 3-pyridyl, etc., Ar2 = Ph, 3-MeOC6H4, 4-FC6H4, 3-, 4-pyridyl, R1R2N, = H2N, piperidino, morpholino, 4-methylpiperidino) and II (Ar2 = Ph, 3-, 4-pyridyl, R1R2N = H2N, morpholino, 4-methylpiperidino), with regards to NK1 and NK2 receptor binding affinity, phys.-chem. characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.
Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship, neurokinin receptor-binding. 658-99-1 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H5F2N, Category: nitriles-buliding-blocks.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts