title: Novel bradykinin-1 antagonists containing a (1,2,3,4-tetrahydro-isoquinolin-1-yl)acetic acid scaffold.
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.
authors: Department of Medical Chemistry, University of Szeged, Szeged, Hungary.
authors: József
authors: J
authors: Huszár
authors: Zoltán
authors: Z
authors: Timár
authors: Krisztina Katalin
authors: KK
authors: Szalai
authors: György
authors: G
authors: Keseru
authors: Ferenc
authors: F
authors: Fülöp
authors: Botond
authors: B
authors: Penke
mesh_terms: D065168:Bradykinin Receptor Antagonists; D002118:Calcium / Q000378:metabolism; D003593:Cytoplasm / Q000378:metabolism; D005470:Fluorometry; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D044005:Tetrahydroisoquinolines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C532284:(1,2,3,4-tetrahydro-isoquinolin-1-yl)acetic acid; D065168:Bradykinin Receptor Antagonists; D044005:Tetrahydroisoquinolines; D002118:Calcium