RESUMO
In the present study we synthesized new methoxy derivatives of trans 2,3-diaryl-2,3-dihydrobenzofurans, starting from suitable trans 2,3-diaryloxiranes, using regio- and stereoselective nucleophilic oxiranyl ring-opening reactions. The compounds were tested as anti-inflammatories in U937 cells. All compounds showed a significant role in inhibiting the NF-κB pathway and were able to restore normal ROS and NO level upon LPS activation. Moreover, regarding inhibition of ACLY, enantioenriched (50% ee) 7a50 showed more potency than the racemic counterpart 7arac, together with a higher reduction of prostaglandin E2 production, thus suggesting a stereoselective interaction in this pathway.
Assuntos
Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , ATP Citrato (pro-S)-Liase/antagonistas & inibidores , Anti-Inflamatórios/síntese química , Benzofuranos/síntese química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Humanos , Estrutura Molecular , Óxido Nítrico/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição RelA/metabolismo , Células U937RESUMO
The composition of 500 foods has been stored in a computer in order to analyse a child's diet. The methodology of operations research is applied to a very simple problem: a diet with only two foods. The geometrical representation of the 'feasible region' and of the 'objective function' is illustrated. One of the analytical methods employable with many variables (foods) is considered. This method was used in trying to find diets allowing for the preferential use of selected foods while respecting recommended dietary allowances, the tastes of the child and other constraints. The theoretical difficulty of transferring this methodology to pediatric dietetics was examined. We solved a simple case utilizing this procedure.
