In the present work a family of novel secnidazole-derived Schiff base compounds and their copper(II) complexes were synthesized. The antimicrobial activities of the compounds were evaluated against clinically important anaerobic bacterial strains. The compounds exhibited in vitro antibacterial activity against Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Parabacteroides distasonis and Fusubacterium nucleatum pathogenic anaerobic bacteria. Upon coordination to copper(II) the antibacterial activity significantly increased in several cases. Some derivatives were even more active than the antimicrobial drugs secnidazole and metronidazole. Therefore, the compounds under study are suitable for in vivo evaluation and the microorganisms should be classified as susceptible to them. Electrochemical studies on the reduction of the nitro group revealed that the compounds show comparable reduction potentials, which are in the same range of the bio-reducible drugs secnidazole and benznidazole. The nitro group reduction potential is more favorable for the copper(II) complexes than for the starting ligands. Hence, the antimicrobial activities of the compounds under study might in part be related to intracellular bio-reduction activation. Considering the increasing resistance rates of anaerobic bacteria against a wide range of antimicrobial drugs, the present work constitutes an important contribution to the development of new antibacterial drug candidates.
Triethylphosphinegold(I) complexes [Au(HL1)P-(CH 2 CH 3 ) 3 ]PF 6 (1), [Au(HL2)P(CH 2 CH 3 ) 3 ]PF 6 (2), and [Au-(HL3)P(CH 2 CH 3 ) 3 ]PF 6 (3) were obtained with (E)-2-(1-(2m e t h y l -5 -All compounds were assayed for their cytotoxic activities against HCT-116 colorectal carcinoma cells under normoxia and hypoxia conditions and against nonmalignant HEK-293 human embryonic kidney cells under normoxia conditions. The thiosemicarbazone ligands HL1-HL3 were inactive against HCT-116 cells under hypoxia but while HL3 was inactive, HL1 and HL2 proved to be cytotoxic to both cell lineages under normoxia conditions. Complexes (1−3) and the triethylphosphinegod(I) precursor proved to be active against both cell lineages in normoxia as well as in hypoxia. While 1 and 3 revealed to be active against HEK-293 and HCT-116 cells, being approximately as active against HCT-116 cells in normoxia as under hypoxia, complex (2) proved to be more active against HCT-116 cells under hypoxia than under normoxia conditions, and more active against HCT-116 cells than against the nonmalignant HEK-293 cells, with the selectivity index, calculated as SI = IC 50HEK-293 /IC 50HCT-116hypoxia , equal to 3.7, similar to the value obtained for the control drug tirapazamine (tirapazamine (TPZ), SI = 4). Although the compounds showed distinct cytotoxic activities, the electrochemical behaviors of HL1-HL3 were very similar, as were the behaviors of complexes (1−3). Complex (2) deserves special interest since it was significantly more active under hypoxia than under normoxia conditions. Hence, in this case, selective reduction of the nitro group in a low oxygen pressure environment, resulting in toxic reactive oxygen species (ROS) and damage to DNA or other biomolecules, might operate, while for the remaining compounds, other modes of action probably occur.
Resumo O surgimento de doenças ocasionadas pelo estresse durante o cultivo de juvenis vem tornando-se comum devido à intensificação dos sistemas de produção, ocorrendo elevada mortalidade e prejuízos econômicos ao produtor. Mediante esse contexto, os probióticos que são um conjunto de micro-organismos vivos, estão sendo utilizados devido à sua capacidade de estabelecer-se e multiplicar-se no intestino do hospedeiro e promover o equilíbrio da microbiota, contribuindo com a sanidade e o desempenho dos peixes principalmente nas primeiras semanas de vida. Objetivou-se avaliar o desempenho de juvenis de tilápias do Nilo alimentados com cepas probióticas e submetidos a desafio sanitário. Foram utilizados 180 juvenis, distribuídos em delineamento inteiramente casualizado, com três tratamentos, quatro repetições e 15 peixes como unidade experimental. Os tratamentos foram: T1 - peixes cultivados em água limpa sem o uso de probiótico; T2 - peixes cultivados em água sob desafio e sem o uso de probiótico e T3 - peixes cultivados em água sob desafio e com o uso de probiótico. Não houve efeito significativo (P>0,05) nos parâmetros de desempenho zootécnico, no consumo de ração e sobrevivência. A utilização de probiótico na ração não mostrou-se hábil para proporcionar melhorias no desempenho, consumo de ração e na sobrevivência de juvenis de tilápias do Nilo no período de 30 dias de cultivo.
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