RESUMO
New series of pyrazole derivatives 3-(furan-2-yl)-4-(5-hydroxy-4H-pyrazol-3-yl)-N-phenylbutanamide 1-5 and imidazole derivatives 3-(furan-2-yl)-3-(1H-imidazol-1-yl)-N-phenylpropanamide 6-10 were synthesized by the Mannich base method. Synthesized compounds 1-10 were confirmed by IR, 1H NMR, 13C NMR, Mass and elemental analysis and further screened for antimicrobial activity.
RESUMO
A series of 1,4-dihydropyridine derivatives (1a-g) were prepared from three compounds condensation reaction of ethylacetoacetate, aromatic aldehyde and ammonium hydroxide. A new series of compounds (2a-g) were prepared from compounds (1a-g) via reaction with thiosemicarbazide using the condensation method. The synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectral and elemental analyses. The synthesized compounds (1a-g) and (2a-g) were also screened for anticoagulant properties.
Assuntos
Anticoagulantes/farmacologia , Coagulação Sanguínea/efeitos dos fármacos , Di-Hidropiridinas/farmacologia , Anticoagulantes/síntese química , Anticoagulantes/química , Di-Hidropiridinas/síntese química , Di-Hidropiridinas/química , Humanos , Estrutura Molecular , Valores de Referência , EstereoisomerismoRESUMO
A series of 1,4-dihydropyridine derivatives (1a-g) were prepared from three compounds condensation of Hantzsch synthesis. A new series of 2,2'-{[4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl}dihydrazinecarbothioamide (2a-g) were prepared from compounds diethyl 4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate (1a-g) reacted with thiosemicarbazide to give the corresponding compounds (2a-g) by hydrazinolysis method. The synthesized compounds were confirmed by IR, (1)HNMR, (13)CNMR, mass spectral and elemental analyses. The newly synthesized compounds (2a-g) were screened for anticonvulsant activity against in swiss albino rat. The test was evaluated by maximal electrode induced convulsion method. Synthesized compounds were used two (50 and 100 mg/kg) concentrations. Compounds (1a-g) were inactive while compounds (2a-g) have moderate anti-convulsant activity compared with standard phenytoin drug. The compound 2,2'-{[4-(furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl} dihydrazinecarbothioamide (2a) has highly active compared with other compound (2b-2g).