Amidoximes are an interesting class of compounds. They can serve as starting materials for the synthesis of valuable heterocyclic and other useful compounds. Their use as starting materials has enabled a wide range of applications in novel pharmaceuticals, antitumor agents, antimalarial agents, nitric oxide synthase (NOS) substrates, enhanced textile materials, synthetic polymers and chelating resins. Concerning the chemistry of amidoximes, during the last 22 years some new methodologies as well as improvements of previously reported reactions appeared in the literature. In this review is discussed the application and methods used for synthesis of amidoximes.
1,2,4-Oxadiazole are compounds that have attracted the attention of many researchers due to their wide range of biological activities. Methods used for the synthesis of 3,5-substituted 1,2,4-oxadiazoles are reviewed in this works, as well as their applications. The syntheses are based mostly on the use of primary amidoximes and acylating agents as the initial reactants. In the last years, numerous reports concerning new methods of synthesis of 1,2,4-oxadiazoles have been reported. The use of microwave irradiation and ultrasound in chemical synthesis has many advantages with consequent impacts on the economy and the environment.
Neste trabalho, é descrito a síntese, caracterização estrutural e atividade antitumoral in vitro de 1,2,4-oxadiazois. As arilamidoximas, produtos de partida de interesse, foram obtidos em bons rendimentos (70-92%). Por outro lado, os 3-aril-(1,2,4-oxadiazol-5-il)-propan-2-ona (5a-c) foram obtidos a partir do acetoacetato de etila com arilamidoxima através do aquecimento durante 4 horas em rendimento de 74-88%. Em seguida os compostos 3a-c foram submetidos a reação de redução com borohidreto de sódio para fornecer os 3-aril-(1,2,4-oxadiazol-5-il)-propan-2-ol (6a-c) em rendimento variando de 75-88%. Compostos contendo o núcleo oxadiazolico da série (5a-c) e (6a-c) foram submetidos a teste biológico para verificação da citoxicidade in vitro dos mesmos frente a células tumorais - HT29 (carcinoma de cólon - humano), HL60 (leucemia promielocítica) e NCI H-292 (câncer de pulmão - humano). Os compostos (5a-c) e (6a-c) tiveram suas atividades antitumoral in vitro testada e 5a/b apresentaram atividade moderada e 5c boa atividade frente as células HL60. Por outro lado, os compostos 6a-c não apresentaram atividades.
Objective: the development of new drugs against Methicillin-resistant Staphylococcus aureus is a priority to the World Health Organization. So, the objective of this study was to evaluate the antibacterial activity and toxicity of 5-bromo-3-((4-methoxyphenyl) sulfenyl)-1H-indole (3b) against MRSA.Methods: minimum inhibitory concentration (MIC) of 3b was determined against S. aureus ATCC 29213 and 43 clinical isolates. The time-kill assay was performed for 9 isolates. Analysis of variance followed by the post hoc Bonferroni test was used for the statistical tests.Results and conclusions: the MIC50 and MIC90 of 3b were 4 μg.mL-1 and 16 μg.mL-1 respectively. In time-kill assay, the 3b showed bactericidal activity to all evaluated isolates at concentrations of 1xMIC and 2xMIC and the re-growth effect was not observed. About the toxicity tests, 3b has not presented cytotoxicity, mutagenicity, or allergenicity. 3b had particularly good activity against MRSA demonstrating high potential for the development of new antimicrobials products.
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