RESUMO
Some new pyrazolo[3,4-b]pyrazines and related heterocycles were synthesized and evaluated for their antifungal and antiparasitic activities. The key intermediate, 6-amino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyrazine-5-carbonitrile (3) was obtained in a one-pot synthesis via the reaction of 5-amino-3-methyl-4-nitroso-1-phenylpyrazole 2 with malononitrile.
Assuntos
Antifúngicos/síntese química , Parasitos/efeitos dos fármacos , Pirazinas/síntese química , Pirazóis/síntese química , Animais , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Leishmania/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Pirazinas/farmacologia , Pirazóis/farmacologia , Espectrofotometria Infravermelho , Trichomonas vaginalis/efeitos dos fármacosRESUMO
The aminoimidazolinyl derivative 3 was synthesized using the pyrazole amino aldehyde 1 as a starting material. Compound 3 has been used as a key intermediate in the synthesis of the title compounds.
Assuntos
Compostos Policíclicos/síntese química , Pirazóis/síntese química , Piridinas/síntese química , Espectroscopia de Ressonância Magnética , Espectrofotometria InfravermelhoRESUMO
2-Acetyl-4-(p-chlorophenyl)-3-(1-pyrrolyl)-5,6,7,8- tetrahydrothieno[2,3-b]quinoline (4a) and its corresponding 2-carbohydrazide derivative 5 were prepared and used as key intermediates in the synthesis of the title compounds. Some of the synthesized compounds were screened for their antibacterial and antifungal activities.
Assuntos
Anti-Infecciosos/síntese química , Quinolinas/síntese química , 4-Quinolonas , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Quinolinas/farmacologia , Relação Estrutura-AtividadeRESUMO
The synthesis of the title heterocycles was achieved using 3-amino-5,6-diphenylpyridazine-4-carbonitrile (4) as a starting material. This compound was converted into the corresponding 4-imidazolinyl derivative 5 which was then subjected to cyclization reactions to afford the title compounds.
Assuntos
Anti-Infecciosos/síntese química , Piridazinas/síntese química , Antibacterianos , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Piridazinas/farmacologiaRESUMO
Sodium dodecyl sulphate- poly acrylamide gel electronphoresis (SDS-PAGE) fractionation of tegumental surface antigens (STEG-Ags.) of 7-day cultured normal and irradiated schistosomula showed no obvious qualitative differences. The observed polypeptide bands of both normal irradiated STEG-Ags. were almost identical and have similar corresponding molecular weights. The immunoblotting assay, using different types of mouse sera, revealed similarity between the bands of both normal and irradiated STEG-Ags. recognized by each type of mouse serum. No qualitative rather than quantitative differences have been observed. The quantitative differences were reflected in intensively staining of some bands from normal STEG-Ag. rather than their corresponding bands of the same molecular weights from irradiated STEG-Ag.
