Pyridazines. XIII. Synthesis of 6-Aryl-5-Oxygenated Substituted-3(2H)-Pyridazinones and Evaluation as Platelet Aggregation Inhibitors

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概要

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• Several 6-aryl-5-oxygenated substituted pyridazinones have been synthesized and evaluated in vitro for inhibition of platelet aggregation induced by adenosine 5'-diphosphate (ADP), thrombin and collagen. All the tested compounds (except 8 and 9) inhibited platelet aggregation in a dose-dependent manner. The IC_<50> of the most active substance, compound 2b, was around 60 μM against ADP and collagen as inducers. The inhibition of platelet aggregation caused by test compounds was dependent on the level of oxidation of the function at the 5-position, with the order of IC_<50> values being R-OH (2a, b, 5)< R-CHO (6,7)≪R-COOH (8,9). None of the tested compounds increased the intracellular levels of cAMP, indicating a lack of inhibitory activity on cAMP phosphodiesterase (PDE III) in intact cells. These results suggest that the group present at the 5 position of 6-aryl-5-substituted pyridazinones determines the platelet aggregation-inhibitory activity, and that a mechanism other than PDE inhibition is responsible for this effect.

• 公益社団法人日本薬学会の論文
• 1997-07-15

著者

• Ravina E

  Lahoratorio De Quimica Farmacciitica Deparhimento De Qitimica Organica Facultud De Farmacia Universi

• Sotelo Eddy

  Lahoratorio De Quimica Farmacciitica Deparhimento De Qitimica Organica Facultud De Farmacia Universi

• SOTELO Eddy

  Laboratorio de Quimica Farmaceutica, Departamento de Quimica Organica, Facultad de Farmacia, Univers

• RAVINA Enrique

  Laboratorio de Quimica Farmaceutica, Departamento de Quimica Organica, Facultad de Farmacia, Univers

• Cano Ernesto

  Departamento De Farmacologia Facultad De Farmacia Universidad De Santiago De Compostela

• Laguna Reyes

  Departamento De Farmacologia Facultad De Farmacia Universidad De Santiago De Compostela

• LAGUNA Reyes

  Laboratorio de Farmacologia Facultad de Farmacia, Universidad de Santiago de Compostela

• CANO Ernesto

  Laboratorio de Farmacologia Facultad de Farmacia, Universidad de Santiago de Compostela

• ESTEVEZ Isabel

  Laboratorio de Quimica Farmaceutica, Facultad de Farmacia, Universidad de Santiago de Compostela

• RODRIGUEZ-LINARED Belen

  Laboratorio de Farmacologia Facultad de Farmacia, Universidad de Santiago de Compostela

• Estevez Isabel

  Laboratorio De Quimica Farmaceutica Facultad De Farmacia Universidad De Santiago De Compostela

• Rosa Elizabeth

  Department Of Pharmacology Faculty Of Pharmacy University

• Rodriguez-linared Belen

  Laboratorio De Farmacologia Facultad De Farmacia Universidad De Santiago De Compostela

• Rodriguez-Linares Belen

  Laboratorio de Farmacologia Facultad de Farmacia, Universidad de Santiago de Compostela

関連論文

• Synthesis of 1-Substituted-6-methyluracils
• Pyridazine Derivatives 32 : Stille-Based Approaches in the Synthesis of 5-Substituted-6-phenyl-3(2H)-pyridazinones
• Pyridazines. Part 31 : Synthesis and Antiplatelet Activity of 4,5-Disubstituted-6-phenyl-3(2H)-pyridazinones
• Pyridazines XVIII. 6-Aryl-3(2H)-Pyridazinones Inhibit Calcium Influx in Stimulated Platelets
• Pyridazines. XIII. Synthesis of 6-Aryl-5-Oxygenated Substituted-3(2H)-Pyridazinones and Evaluation as Platelet Aggregation Inhibitors
• Synthesis and Affinities for Dopamine (D_2) and 5-Hydroxytryptamine (5-HT_) Receptors of 1-(Benzoylpropyl)-4-(1-oxocycloalkyl-2-ethyl)-piperazines as Cyclic Butyrophenone Derivatives
• Piperazinomethyl Tetralines : Synthesis and Affinities for D_1,D_2 and 5-HT_ Receptors
• 1,5-Dimethyl-6H-pyridazino [4,5-b] carbazole, a 3-Aza Bioisoster of the Antitumor Alkaloid Olivacine

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