| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378364 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
SAR study of the biphenyl region of 2,3-diaminopyridine bradykinin B1 antagonists was investigated with non-aromatic carbo- and heterocyclic rings. A piperidine ring was found to be a good replacement for the proximal phenyl ring while replacement of the distal phenyl was optimal with a cyclohexyl group leading to a dramatic improvement in affinity for the B1 receptor.
Graphical abstractAn SAR analysis of 2,3-diaminopyridine bradykinin B1 antagonists was carried out and revealed that either of the aromatic rings comprising the biphenyl region could be effectively replaced with non-aromatic carbo- or heterocyclic rings.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Scott D. Kuduk, Ronald K. Chang, Christina Ng, Kathy L. Murphy, Richard W. Ransom, Cuyue Tang, Thomayant Prueksaritanont, Roger M. Freidinger, Douglas J. Pettibone, Mark G. Bock,