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.
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. vbodmer@mac.com
Vera
V
Bodmer-Narkevitch
Neville J
NJ
Anthony
Victoria
V
Cofre
Samson M
SM
Jolly
Kathy L
KL
Murphy
Richard W
RW
Ransom
Duane R
DR
Reiss
Cuyue
C
Tang
Thomayant
T
Prueksaritanont
Douglas J
DJ
Pettibone
Mark G
MG
Bock
Scott D
SD
Kuduk
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