| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366400 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B1 antagonists was examined. Incorporation of a pyridine in place of the proximal phenyl ring and chlorination of the distal phenyl ring proved to be well tolerated and provided compounds with improved pharmacokinetic profiles, CNS penetration, and enhanced receptor occupancy.
Graphical abstractSAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B1 antagonists was examined.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Scott D. Kuduk, Robert M. DiPardo, Ronald K. Chang, Christina N. Di Marco, Kathy L. Murphy, Richard W. Ransom, Duane R. Reiss, Cuyue Tang, Thomayant Prueksaritanont, Douglas J. Pettibone, Mark G. Bock,