RESUMEN

Nafuredin-γ (2), converted from nafuredin (1) under mild basic conditions, demonstrates potent and selective inhibitory activity against helminth complex I. However, 2 is unstable in air because the conjugated dienes are oxygen-labile. To address this, we designed and synthesized air-stable nafuredin-γ analogs. Although the complex I inhibitory activities of all the new nafuredin-γ analogs were lower than that of 2, all were in the high nM range (IC50: 300-820nM).

Asunto(s)

Diseño de Fármacos , Complejo I de Transporte de Electrón/antagonistas & inhibidores , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Pironas/química , Pironas/farmacología , Aire , Estabilidad de Medicamentos , Inhibidores Enzimáticos/síntesis química , Concentración 50 Inhibidora , Pironas/síntesis química