2,3-Diaminopyridine Bradykinin B1 Receptor Antagonists

Autor: Kuduk, S. D., Ng, C., Feng, D.-M., Wai, J. M.-C., Chang, R. S. L., Harrell, C. M., Murphy, K. L., Ransom, R. W., Reiss, D., Ivarsson, M., Mason, G., Boyce, S., Tang, C., Prueksaritanont, T., Freidinger, R. M., Pettibone, D. J., Bock, M. G.
Zdroj: Journal of Medicinal Chemistry; December 2004, Vol. 47 Issue: 26 p6439-6442, 4p
Abstrakt: 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.
Databáze: Supplemental Index