565460-54-0Relevant 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.
Development of an efficient and selective radioligand for bradykinin B 1 receptor occupancy studies
Su, Dai-Shi,Markowitz, M. Kristine,Murphy, Kathy L.,Wan, Bang-Lin,Zrada, Matthew M.,Harrell, C. Meacham,O'Malley, Stacy S.,Hess, J. Fred,Ransom, Rick W.,Chang, Ray S.,Wallace, Michael A.,Raab, Conrad E.,Dean, Dennis C.,Pettibone, Douglas J.,Freidinger, Roger M.,Bock, Mark G.
, p. 6045 - 6048 (2007/10/03)
We have developed an efficient and selective radioligand, the [ 35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in transgenic rats over-expressing the human bradykinin B1 receptor.
NOVEL QUINOXALINONE DERIVATIVES AS BRADYKININ B1 ANTAGONISTS
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Page/Page column 26-27, (2010/02/07)
2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Discovery of a potent, non-peptide bradykinin B1 receptor antagonist
Su, Dai-Shi,Markowitz, M. Kristine,DiPardo, Robert M.,Murphy, Kathy L.,Harrell, C. Meacham,O'Malley, Stacy S.,Ransom, Richard W.,Chang, Raymond S. L.,Ha, Sookhee,Hess, Fred J.,Pettibone, Douglas J.,Mason, Glenn S.,Boyce, Susan,Freidinger, Roger M.,Bock, Mark G.
, p. 7516 - 7517 (2007/10/03)
Bradykinin (BK) plays an important role in the pathophysiological processes accompanying pain and inflammation. Selective bradykinin B1 receptor antagonists have been shown to be anti-nociceptive in animal models and could be novel therapeutic
SULFONYLQUINOXALONE ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ ANTAGONISTS
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Page/Page column 113, (2010/02/07)
Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists to relieve symptons, associated with bradykinin including pain, inflammation, bronchoconstriction, cerebral edema, etc.
