Indazole derivatives as novel bradykinin B1 receptor antagonists

Vera Bodmer-Narkevitch; Neville J Anthony; Victoria Cofre; Samson M Jolly; Kathy L Murphy; Richard W Ransom; Duane R Reiss; Cuyue Tang; Thomayant Prueksaritanont; Douglas J Pettibone; Mark G Bock; Scott D Kuduk

doi:10.1016/j.bmcl.2010.09.121

Indazole derivatives as novel bradykinin B1 receptor antagonists

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7011-4. doi: 10.1016/j.bmcl.2010.09.121. Epub 2010 Sep 29.

Authors

Vera Bodmer-Narkevitch¹, Neville J Anthony, Victoria Cofre, Samson M Jolly, Kathy L Murphy, Richard W Ransom, Duane R Reiss, Cuyue Tang, Thomayant Prueksaritanont, Douglas J Pettibone, Mark G Bock, Scott D Kuduk

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]

PMID: 20971001
DOI: 10.1016/j.bmcl.2010.09.121

Abstract

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.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1
Bradykinin B1 Receptor Antagonists*
Humans
Indazoles / pharmacokinetics
Indazoles / pharmacology*
Protein Binding
Structure-Activity Relationship

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Bradykinin B1 Receptor Antagonists
Indazoles