RESUMO
Fourteen new potentially biologically active 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were synthesized and characterized by elemental analysis, 1H NMR, IR and UV spectra. Three of these compounds were screened for their antitumor activities.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Células Tumorais CultivadasRESUMO
Reactions of 3-amino-1,2,4-triazole with some dicarboxylic acid anhydrides and diketones were studied. The structural assignments of the compounds obtained from the reactions are based on elemental analyses and spectral data. The compounds were screened for their in vitro antibacterial activities.
Assuntos
Anti-Infecciosos/farmacologia , Ácidos Dicarboxílicos/química , Cetonas/química , Triazóis/síntese química , Triazóis/farmacologia , Antituberculosos/farmacologia , Testes de Sensibilidade Microbiana , Microquímica , Relação Estrutura-AtividadeRESUMO
Nine new 1,3,4-trisubstituted-4,5-dihydro-1H-1,2,4-triazol-5-ones were synthesized and characterized by elemental analysis, 1H NMR, IR and UV spectra. These new and 30 recently reported 3,4-disubstituted- and 1,3,4-trisubstituted-4,5-dihydro-1H-1,3,4-triazol-5-ones were screened for antibacterial, antitumor and anti-HIV activities.
Assuntos
Cetonas/síntese química , Triazóis/síntese química , Cetonas/farmacologia , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , Triazóis/farmacologiaRESUMO
The cyclization of ester thiosemicarbazones to two different heterocycles was studied for some new thiosemicarbazones, and only the formation of 1,2,4-triazol-5-thiols was attributed to the regioselectivity of the ring closure reaction, due to a steric hindrance of bulky groups. Next, some of the new compounds were tested for their in vitro antimicrobial and antitumor activities.
Assuntos
Antibióticos Antituberculose/síntese química , Antineoplásicos/síntese química , Tiossemicarbazonas/síntese química , Antibióticos Antituberculose/farmacologia , Antineoplásicos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Tiossemicarbazonas/farmacologia , Triazóis/síntese química , Triazóis/farmacologia , Células Tumorais Cultivadas/efeitos dos fármacosRESUMO
Twenty-one new 1-methyl- and 1-ethyl-3,4-disubstituted-4,5-dihydro- 1H-1,2,4-triazol-5-ones were synthesized and characterised by elemental analysis, 1H-NMR and IR spectra. These new and 16 recently reported derivatives of 4,5-dihydro-1H-1,2,4-triazol-5-one ring were screened for their antibacterial activities.
Assuntos
Antibacterianos/síntese química , Triazóis/síntese química , Antibacterianos/farmacologia , Antituberculosos/síntese química , Antituberculosos/farmacologia , Bactérias/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Espectrofotometria Ultravioleta , Triazóis/farmacologiaRESUMO
A series of 3-alkyl/aryl-4-arylidenamimo-4,5-dihydro-1H-1,2,4- triazol-5-ones was synthesized and characterized by elemental and spectral analysis. These compound were tested for in vitro antibacterial and antifungal activity in solid agar cultures against eight microorganisms. In these test, some of the new compounds were shown to be very potent in vitro antifungal activity against the used fungi.
Assuntos
Antifúngicos/síntese química , Fungos/efeitos dos fármacos , Triazóis/síntese química , Antifúngicos/farmacologia , Testes de Sensibilidade Microbiana , Triazóis/química , Triazóis/farmacologiaRESUMO
Eight new 3-alkyl(aryl)-4-arylidenamino-4,5-dihydro-1H-1,2,4-triazol-5 - ones were synthesized and characterised by elemental analysis. 1H NMR, IR and UV spectra. Seven new and 34 recently reported derivatives of 4,5-dihydro-1H-1,2,4 triazol-5-one ring were screened for their antitumor activities.
Assuntos
Antineoplásicos/síntese química , Triazóis/síntese química , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Triazóis/farmacologia , Células Tumorais CultivadasRESUMO
Reactions of 3-substituted-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones [I] with some arenesulfonyl chlorides and aryl isocyanates were studied and the corresponding N-(3-substituted-4,5,-dihydro-1H-1,2,4-triazol-5-one-4-yl) arenesulfonamides [II-VI] and N-aryl-N-(3-substituted-4,5-dihydro-1H-1,2,4-triazol-5-one-4-yl) ureas [V, VI] were obtained. The structural assignments of new 19 compounds are based on spectral data and elemental analysis. Furthermore, compounds II-VI were tested for their in vitro antimicrobial activities.
Assuntos
Antibacterianos/síntese química , Naftalenossulfonatos/síntese química , Sulfonamidas/síntese química , Ureia/química , Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Isocianatos/química , Testes de Sensibilidade Microbiana , Naftalenossulfonatos/farmacologia , Relação Estrutura-Atividade , Sulfonamidas/farmacologiaRESUMO
The reactions of 3-alkyl(aryl)-4-phenylamino-4,5-dihydro-1H-1,2,4-triazol-5-ones with appropriate alkyl halides via sodio derivatives were studied and the corresponding 1-alkyl-3-alkyl(aryl)-4-phenylamino-4,5-dihydro-1H-1,2,4-traizol-5 -ones were synthesized. Next, the new compounds were tested for their in vitro antimicrobial activities.