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New Pyrimido[5,4‐c]cinnolines with Antiplatelet Activities
Author(s) -
Rehse Klaus,
Gonska Hedwig
Publication year - 2005
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.200500152
Subject(s) - chemistry , antagonist , antagonism , platelet aggregation , stereochemistry , aspirin , platelet , ring (chemistry) , pharmacology , biochemistry , receptor , organic chemistry , medicine
Twenty one new pyrimido[5,4‐c]cinnolines containing different lipophilic moieties (viz. phenyl, 4‐methoxyphenyl, 2‐furanyl, 2‐thienyl) in position 2 and additional basic groups ( e.g. , alkylaminopropyl, dialkylaminopropyl and cyclohexylaminopropyl) in position 4 of the title ring system have been prepared and investigated for antiplatelet effects (Born test). Ten of them inhibited the platelet aggregation induced by collagen with an IC 50 below 10 μmol/L ( 6a , 6b , 6c , 6g , 6h , 6i , 6k , 6m , 6q , 6u ). A closer inspection of the antiplatelet effect with other inducers showed antagonism against adrenaline ( 6m ), ADP antagonist ( 6i ) and PAF antagonist activities ( 6m , 6i , 6u ) in nanomolar (IC 50 ) concentration ranges.