RESUMO
In this study, a series of novel 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a-g) and 1,3,4-oxadiazole (7a-g, 8) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (-) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5-100 µg/mL in DMSO. It has been observed that triazolo-thiadiazole derivatives are found to be more active than 1,3,4-oxadiazole derivatives against all pathogenic bacterial and fungal strains.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Benzotiazóis/farmacologia , Fungos/efeitos dos fármacos , Hidrazinas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Benzotiazóis/síntese química , Benzotiazóis/química , Relação Dose-Resposta a Droga , Hidrazinas/síntese química , Hidrazinas/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a-t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds displayed good anticonvulsant activity with lesser neurotoxicity. To assess the unwanted effects of the compounds on liver, estimation of enzymes and proteins was carried out.
Assuntos
Anticonvulsivantes/farmacologia , Anticonvulsivantes/toxicidade , Avaliação Pré-Clínica de Medicamentos/métodos , Pirimidinas/química , Semicarbazonas/farmacologia , Semicarbazonas/toxicidade , Animais , Anticonvulsivantes/síntese química , Anticonvulsivantes/química , Sinergismo Farmacológico , Epilepsia/tratamento farmacológico , Fígado/efeitos dos fármacos , Fígado/enzimologia , Fígado/metabolismo , Camundongos , Sistema Nervoso/efeitos dos fármacos , Semicarbazonas/síntese química , Semicarbazonas/químicaRESUMO
A series of quinoxalinone derivatives was synthesized by the condensation of 1,2-diaminobenzene with alpha-ketoglutaric acid to yield 3-(3-oxo-3,4-dihydroquinoxalin-2-yl) propionic acid (2) and then treated with hydrazine hydrate to yield its hydrazones (3). This was further reacted with substituted aromatic aldehydes to produce final compounds (4a-r). These hydrazones derivatives were characterized by FT-IR and 1H-NMR data. All the synthesized compounds were evaluated for their antimicrobial and antiinflammatory activity.
Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/farmacologia , Hidrazonas/síntese química , Hidrazonas/farmacologia , Quinoxalinas/síntese química , Quinoxalinas/farmacologia , Animais , Carragenina , Edema/induzido quimicamente , Edema/prevenção & controle , Escherichia coli/efeitos dos fármacos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Ratos , Espectrofotometria Infravermelho , Staphylococcus aureus/efeitos dos fármacosRESUMO
A series of 1,2,4-triazine derivatives Va (1-24) and Vb (1-24) were synthesized and evaluated for their anti-anxiety and anti-inflammatory activities. The structures of the synthesized compounds were confirmed on the basis of their spectral data. Many of the triazine compounds were found to possess good activity. Especially, compounds bearing the sulfur atom showed better activity than those bearing the oxygen atom.
