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Bradykinin B1 antagonists : Biphenyl SAR studies in the cyclopropanecarboxamide series
SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B(1) 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 p...
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Published in: | Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (13), p.3608-3612 |
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Main Authors: | , , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B(1) 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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2007.04.040 |