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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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (13), p.3608-3612
Main Authors: KUDUK, Scott D, DIPARDO, Robert M, BOCK, Mark G, CHANG, Ronald K, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J
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Language:English
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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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.040