✍ Scribed by Klaus Rehse; Tobias Baselt
No coin nor oath required. For personal study only.
In the Born test, 23 title compounds were synthesized and investigated 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 10 μM were found (3a, 3b, 3c) and 15 compounds with IC~50~ values between 10 and 100 μM were determined. In general, a cyclohexylamino rest on an 4‐carboxamide moiety is a pre‐requisite for this pharmacological activity. A clear dependence from the substituent R^1^ in the structural element Y is observed. The same is true for the spacer n in the 4‐carboxamide substituent. Compound 3e showed strong ADP‐antagonistic effects (IC~50~ = 2.2 nM); 3c antagonized adrenaline (IC~50~ = 2.8 nM), while 3n was highly effective against platelet‐activating factor (IC~50~ = 0.2 μM).
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## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
## Abstract 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 sys
## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.