Indazole derivatives as novel bradykinin B1 receptor antagonists.
A new class of indazole-derived bradykinin B(1) antagonists and their structure-activity relationships (SAR) is reported. A number of compounds were found to have low-nanomolar affinity for the human B(1) receptor and possess acceptable P-gp and pharmacokinetics properties.
Bodmer-Narkevitch
Vera
V
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. vbodmer@mac.com
Anthony
Neville J
NJ
Cofre
Victoria
V
Jolly
Samson M
SM
Murphy
Kathy L
KL
Ransom
Richard W
RW
Reiss
Duane R
DR
Tang
Cuyue
C
Prueksaritanont
Thomayant
T
Pettibone
Douglas J
DJ
Bock
Mark G
MG
Kuduk
Scott D
SD
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D065169:Bradykinin B1 Receptor Antagonists; D006801:Humans; D007191:Indazoles / Q000493:pharmacokinetics / Q000494:pharmacology*; D011485:Protein Binding; D013329:Structure-Activity Relationship
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D065169:Bradykinin B1 Receptor Antagonists; D007191:Indazoles