Novel bradykinin-1 antagonists containing a (1,2,3,4-tetrahydro-isoquinolin-1-yl)acetic acid scaffold |
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Authors: | Huszár József Timár Zoltán Szalai Krisztina Katalin Keseru György Fülöp Ferenc Penke Botond |
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Institution: | Department of Medical Chemistry, University of Szeged, Szeged, Hungary. |
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Abstract: | 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. |
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Keywords: | Bradykinin-1 receptor B1 antagonist Bradykinin Isoquinoline Peptidomimetic |
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