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Quinolizidinyl‐benzimidazoles as Platelet‐Antiaggregating Agents
Author(s) -
Vazzana Iana,
Terranova Emanuela,
Tasso Bruno,
Tonelli Michele,
Piana Antonietta,
Gastaldi Stefanella,
Sparatore Fabio
Publication year - 2008
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200890068
Subject(s) - chemistry , epimer , agonist , benzimidazole , platelet aggregation , selectivity , platelet , stereochemistry , receptor , biochemistry , medicine , organic chemistry , catalysis
Two series of (±)‐2‐phenyl‐1‐(quinolizidin‐1 α ‐yl)benzimidazoles, 12A – 26A , and (±)‐2‐phenyl‐1‐(quinolizidin‐1 β ‐yl)benzimidazoles, 12B – 26B , were prepared and tested for the inhibition of human platelets aggregation induced by ADP, collagen, and adrenaline. All epimers A , i.e. , 12A – 26A , were devoid of any activity against the three agonists, while the epimers B , i.e. , 12B – 26B , exhibited different degrees of activity, though practically confined against the ADP‐induced aggregation. The best compounds were 19B, 24B , and 26B , which inhibited for 69–67% at 260 μ M and for 40–29% at 65 μ M concentration the ADP (2 μ M )‐induced aggregation. The observed agonist and spatial structure selectivity warrant further investigations of this kind of benzimidazole derivatives.