1.
Bioorg Med Chem Lett
; 49: 128264, 2021 10 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-34280408
RESUMEN
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.
Asunto(s)
Antiinflamatorios/farmacología , Benzofuranos/farmacología , ATP Citrato (pro-S)-Liasa/antagonistas & inhibidores , Antiinflamatorios/síntesis química , Benzofuranos/síntesis química , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Humanos , Estructura Molecular , Óxido Nítrico/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Transducción de Señal/efectos de los fármacos , Factor de Transcripción ReIA/metabolismo , Células U937
2.
Eur J Neurol
; 21(3): e25-6, 2014 Mar.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24517879