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Biol Pharm Bull ; 25(6): 798-802, 2002 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12081151

RESUMO

In the present study, a series of 2-substituted-4-methyl-7-amino/4,7-dimethyl-1,8-naphthyridines were synthesized and characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant (125, 250 mg/kg), cardiac and antimicrobial activities. The compounds were screened for antibacterial activity against gram (+) bacteria (Staphylococcus epidermidis, Bacillus subtilis, Enterococcusfaecalis and Micrococcus luteus) and gram (-) bacteria (Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli and Salmonella typhi). All the compounds except 2-(3'-phenylaminopropyloxy)-4-methyl-7-amino-1,8-naphthyridine exhibited significant anticonvulsant activity. The anticonvulsant activity of 2-(3-morpholino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine, 2-(3'-diphenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine and 2-(3'-diethanolamino-propyloxy)-4,7-dimethy-1,8-naphthyridine at the dose of 250 mg/kg were found to be equivalent to diazepam (5 mg/kg). Sympathetic blocking activity was observed with 2-(3'-phenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine, 2-(3'-diethanolamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine and 2-(3'-diphenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine only. All the compounds were devoid of antibacterial activity against the tested bacteria.


Assuntos
Antiarrítmicos/síntese química , Antiarrítmicos/farmacologia , Antibacterianos/síntese química , Antibacterianos/farmacologia , Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Naftiridinas/síntese química , Naftiridinas/farmacologia , Animais , Relação Dose-Resposta a Droga , Eletrochoque , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Coração/efeitos dos fármacos , Técnicas In Vitro , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Naftiridinas/química , Ranidae , Ratos , Ratos Wistar , Espectrofotometria Infravermelho , Espectroscopia de Infravermelho com Transformada de Fourier
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