Synthesis, antiplatelet activity and comparative molecular field analysis of substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones, their congeners and isosteric analogues.

doi:10.1016/S0968-0896(00)00010-9

Paper

Synthesis, antiplatelet activity and comparative molecular field analysis of substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones, their congeners and isosteric analogues.

Published Apr 1, 2000 · G. Roma, N. Cinone, M. Di Braccio

Bioorganic & medicinal chemistry

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Abstract

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In Vitro Study

Study Snapshot

Substitution derivatives of 2-amino-4H-pyrido[1,2-a]pyrimidin-4-one show near-identical antiplatelet activity when induced by ADP or A23187, but less active when induced by collagen.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis, antiplatelet activity and comparative molecular field analysis of substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones, their congeners and isosteric analogues.

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References

Effect of 2-(1-piperazinyl)-4H-pyrido[1,2-a]pyrimidin-4-one (AP155) on human platelets in vitro.

AP155 effectively inhibits platelet aggregation by increasing cAMP intracellular concentration, effectively reducing platelet activation and thrombin-induced calcium levels.

Pyran derivatives XIX. (Dialkylamino) substituted 1-benzopyranones and naphthopyranones with platelet antiaggregating activity.

7-Ethoxy-4-(1-piperazinyl)coumarin 11b shows the highest antiplatelet activity, surpassing all reference compounds and showing higher activity than ASA, trifluoperazine, propranolol, and dipyridamole.

Molecular Lipophilicity Potential, a tool in 3D QSAR: Method and applications

The new method for calculating Molecular Lipophilicity Potential (MLP) can be used as a third field in CoMFA studies, providing insights into ligand-receptor interactions.

1,2-fused pyrimidines. VI. Substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones with antiplatelet activity.

Substituted 2-amino-4H-pyrido[1,2-a]pyrimidine-4-ones show antiplatelet activity, with the most active compounds being 2 g and 2 b, both targeting ADP and collagen, respectively.

Mode of action of 2‐(diethylamino)‐7‐ethoxychromone on human platelets

RC39XVIII inhibits platelet aggregation, thromoboxane B2 formation, and granule release, while potentiating cAMP accumulation and inhibiting soluble cAMP phosphodiesterase.

Citations

Electro-Oxidative C3-Selenylation of Pyrido[1,2-a]pyrimidin-4-ones

Electrochemically driven external oxidant-free strategies can effectively achieve C3-selenylation of pyrido[1,2-a]pyrimidin-4-ones, yielding diverse seleno-substituted N-heterocycles in moderate to excellent yields.

Synthesis of polyfunctional fluoro-quinoline and fluoro-pyridopyrimidinone derivatives

Selectively fluorinated heterocycles can be rapidly synthesized using 2-Fluoromalonic acid and phosphoryl chloride, leading to a library of 30 novel polysubstituted derivatives with diverse substituents.

Thiocarbonylation of C(sp3)-H bonds in pyridylamines with CS2: Facile synthesis of pyrido[1,2-a]pyrimidine-4-thiones

This study presents a facile synthesis of pyrido[1,2-a]pyrimidine-4-thiones using carbon disulfide, offering high yields, scalability, and atom economy.

Metal free C-3 chalcogenation (sulfenylation and selenylation) of 4H-pyrido[1,2-a]pyrimidin-4-ones

This metal-free C-3 chalcogenation of 4H-pyrido[1,2-a]pyrimidin-4-one effectively synthesizes diverse 3-ArS/ArSe derivatives in high yields (up to 95%) under mild conditions and broad functional group tolerance.

An efficient one-pot synthesis of highly functionalized benzylpyrazolyl pyrido[1,2-a]pyrimidine derivatives using CuFe2O4 nanoparticles under solvent-free conditions

CuFe2O4 nanoparticles efficiently synthesize novel benzylpyrazolyl pyrido[1,2-a]pyrimidine derivatives under solvent-free conditions, offering a green and environmentally friendly method for their synthesis.