Premium
New 1 H ‐Pyrazole‐4‐Carboxamides with Antiplatelet Activity
Author(s) -
Rehse Klaus,
Kotthaus Joscha,
Khadembashi Laleh
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800181
Subject(s) - chemistry , platelet , pyrazole , platelet activating factor , platelet aggregation , stereochemistry , platelet aggregation inhibitor , pharmacology , aspirin , biochemistry , medicine
Nine title compounds were synthesized and investigated in the Born test for their antiplatelet activities against collagen, ADP, adrenaline, and platelet activating factor (PAF) as inducers of the aggregation. Using collagen three compounds with IC 50 values below 100 μM were found ( 3b , 3e , 3i ). Activities in nanomolar concentrations were observed against ADP ( 3b , IC 50 = 9.4 nM), adrenaline ( 3i , IC 50 = 5.8 nM), and platelet activating factor ( 3e , IC 50 = 0.45 nM).