Novel bradykinin-1 antagonists containing a (1,2,3,4-tetrahydro-isoquinolin-1-yl)acetic acid scaffold

A novel B 1 antagonist core was utilized and the effects of modification of its amide side chain on the biological activity were tested. The imino functional group of isoquinolin-1-ylacetic acid and its 6,7-dimethoxy variant was sulfonylated (4-toluenesulfonyl), while the acetyl side chain was converted to amides. Three of the synthesized compounds exhibited significant activity at the recombinant human B 1 receptors in binding tests and also in a functional assay. Novel B 1 antagonist core 1,2,3,4-tetrahydroisoquinolin-1-ylacetic acid was utilized and the effect of modification of its amide side chain on the biological activity was tested. [Display omitted]