Potent bradykinin B 1 receptor antagonists: 4-Substituted phenyl cyclohexanes

4-Substituted phenyl cyclohexanes were identified as alternative isosteres for the biphenyl moiety of the lead compound 1. The syntheses, SAR optimization, and pharmacokinetic profiles of these compounds are described. Selective bradykinin (BK) B 1 receptor antagonists have been shown to be antinoci...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 11; pp. 3006 - 3009
Main Authors Su, Dai-Shi, Lim, John L., Markowitz, M. Kristine, Wan, Bang-Lin, Murphy, Kathy L., Reiss, Duane R., Harrell, C. Meacham, O’Malley, Stacy S., Ransom, Rick W., Chang, Raymond S.L., Pettibone, Douglas J., Tang, Cuyue, Prueksaritanont, Thomayant, Freidinger, Roger M., Bock, Mark G.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.06.2007
Subjects
4-Substituted phenyl cyclohexanes
B 1 receptor
B 1 receptor antagonists
Bradykinin
4-Substituted phenyl cyclohexanes
B 1 receptor antagonists
Bradykinin
B 1 receptor
Online AccessGet full text

Cover

More Information
Summary:4-Substituted phenyl cyclohexanes were identified as alternative isosteres for the biphenyl moiety of the lead compound 1. The syntheses, SAR optimization, and pharmacokinetic profiles of these compounds are described. Selective bradykinin (BK) B 1 receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure–activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B 1 receptor antagonists.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.03.059