Synthesis, antibacterial, anthelmintic and anti-inflammatory studies of novel methylpyrimidine sulfonyl piperazine derivatives
| Autor: | Mohan,Nadigar R., Sreenivasa,Swamy, Manojkumar,Karikere E., Rao,Tadimety M. C., Thippeswamy,Boreddy S., Suchetan,Parameshwar A. |
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| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: | |
| Zdroj: | Journal of the Brazilian Chemical Society, Volume: 25, Issue: 6, Pages: 1012-1020, Published: JUN 2014 Journal of the Brazilian Chemical Society v.25 n.6 2014 Journal of the Brazilian Chemical Society Sociedade Brasileira de Química (SBQ) instacron:SBQ |
| Popis: | A strategic synthesis of novel methylpyrimidine sulfonyl piperazines involving Suzuki coupling was designed and pharmacological activities of the compounds were evaluated. Reactions were carried out under conventional method and show good functional group transformations and high yields. Structures of the newly synthesized compounds were established by infrared spectroscopy (IR), ¹H and 13C nuclear magnetic resonance (NMR) and liquid chromatography-mass spectrometry (LC-MS) and elemental analysis. The compounds were tested for in vitro antibacterial activity against Escherichia coli and Staphylococcus aureus bacterial strains, anthelmintic activity using Pheretima posthuma and anti-inflammatory activity involving carrageenan induced rat paw edema model. Some compounds were proven to be potent pharmacophores. Uma síntese estratégica de novas piperazinas sulfonil metilpirimidina envolvendo acoplamento Suzuki foi desenvolvida e as atividades farmacológicas dos compostos foram avaliadas. As reações foram realizadas pelo método convencional e apresentaram boas transformações dos grupos funcionais e elevados rendimentos. As estruturas dos novos compostos sintetizados foram estabelecidas por espectroscopia no infravermelho (IR), ressonância magnética nuclear (NMR) de ¹H e de 13C, e cromatografia líquida-espectrometria de massas (LC-MS) e análise elementar. Os compostos foram testados quanto à atividade antibacteriana in vitro contra as cepas bacterianas Escherichia coli e Staphylococcus aureus, à atividade antihelmíntica utilizando Pheretima posthuma e à atividade anti-inflamatória envolvendo o modelo de edema de pata de rato induzido pela carragena. Provou-se que alguns compostos são farmacóforos potentes. |
| Databáze: | OpenAIRE |
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