Related Experiment Video
Updated: Aug 14, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
New pyrimido[5,4-c]cinnolines with antiplatelet activities
1Institut für Pharmazie, Freie Universität Berlin, Germany. rehiwer@zedat.fu-berlin.de
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 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 micromol/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.
Related Concept Videos
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Antianginal Drugs: Calcium Channel Blockers and Ranolazine
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
Five-Membered Heterocyclic Aromatic Compounds: Overview
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Basicity of Heterocyclic Aromatic Amines
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
