1053196-27-2Relevant academic research and scientific papers
Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists
Chen, Jian Jeffrey,Qian, Wenyuan,Biswas, Kaustav,Viswanadhan, Vellarkad N.,Askew, Benny C.,Hitchcock, Stephen,Hungate, Randall W.,Arik, Leyla,Johnson, Eileen
scheme or table, p. 4477 - 4481 (2009/04/08)
Replacement of the core β-amino acid in our previously reported piperidine acetic acid and β-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most potent compounds from this series have IC50s a human B1 receptor functional assay. A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.
