- 2,3-diaminopyridine bradykinin B1 receptor antagonists.
2,3-diaminopyridine bradykinin B1 receptor antagonists.
Journal of medicinal chemistry (2004-12-14)
Scott D Kuduk, Christina Ng, Dong-Mei Feng, Jenny M-C Wai, Raymond S L Chang, Charles M Harrell, Kathy L Murphy, Richard W Ransom, Duane Reiss, Magnus Ivarsson, Glenn Mason, Susan Boyce, Cuyue Tang, Thomayant Prueksaritanont, Roger M Freidinger, Douglas J Pettibone, Mark G Bock
PMID15588075
摘要
Bradykinin B1 receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. A series of 2,3-diaminopyridine B1 antagonists was optimized to have sub-nanomolar affinity and good pharmacokinetic properties. Lead compounds were shown to exhibit good efficacy in rabbit in vivo models of pain and inflammation.
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