Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists
…, RM DiPardo, KL Murphy, RW Ransom…
文献索引：Kuduk, Scott D.; Di Marco, Christina N.; Chang, Ronald K.; Wood, Michael R.; Schirripa, Kathy M.; Kim, June J.; Wai, Jenny M. C.; DiPardo, Robert M.; Murphy, Kathy L.; Ransom, Richard W.; Harrell, C. Meacham; Reiss, Duane R.; Holahan, Marie A.; Cook, Jacquelynn; Hess, J. Fred; Sain, Nova; Urban, Mark O.; Tang, Cuyue; Prueksaritanont, Thomayant; Pettibone, Douglas J.; Bock, Mark G. Journal of Medicinal Chemistry, 2007 , vol. 50, # 2 p. 272 - 282
A series of biphenylaminocyclopropane carboxamide based bradykinin B1 receptor antagonists has been developed that possesses good pharmacokinetic properties and is CNS penetrant. Discovery that the replacement of the trifluoropropionamide in the lead structure with polyhaloacetamides, particularly a trifluoroacetamide, significantly reduced P- glycoprotein mediated efflux for the series proved essential. One of these novel bradykinin ...
