A novel series of 2-ethyl-1-(4-substituted)phenyl-1H-imidazole derivatives was designed, synthesized, and tested for its antibacterial activity against various bacterial strains. Most of the synthesized compounds showed potent inhibition of several Gram-positive and Gram-negative bacterial strains with minimum inhibitory concentration (MIC) values in the range of 4-256 nmol mL-1 in vitro. The compound [2-ethyl-1-(4-pentoxy)phenyl-1H-imidazole] exhibited the most potent inhibitory activity. The MIC of this compound against S. aureus was found to be 8 nmol mL-1, smaller than that of the reference agents, ciprofloxacin and amoxicillin. Furthermore, the compound exhibited modest activity against several bacterial strains in a dose range of 8-256 nmol mL-1.

Neste estudo, uma nova série de derivados de 4H-[1,2,4]triazina[3,4-a]ftalazin-4-ona substituídos em C-7 foi sintetizada como potenciais agentes anticonvulsivantes. Suas atividades anticonvulsivantes foram avaliadas pelo teste do eletrochoque máximo (MES), e suas neurotoxicidades, pelo teste 'rotarod' de neurotoxicidade. Os resultados farmacológicos mostraram que a 7-hexiloxi-4H-[1,2,4]triazina[3,4-a]ftalazin-4-ona, 4e, foi a mais potente, com dose efetiva (ED50) de 6,6 mg kg-1 e dose tóxica mediana (TD50) de 39,4 mg kg-1, proporcionando um índice de proteção (PI=TD50 /ED50) de 6,0.

In this study, a novel series of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 7-hexyloxy-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one 4e was the most potent with median effective dose (ED50) value of 6.6 mg kg-1, median toxicity dose (TD50) of 39.4 mg kg-1, providing a protective index (PI=TD50 /ED50) value of 6.0.