Aromatic Regions Govern the Recognition of NADPH Oxidase Inhibitors as Diapocynin and its Analogues

In conclusion, targeting the aromatic region of p47phox through π‐interactions is important for inhibiting NOX activity.

Compound C8, one of the 18 designed compounds with chemical relationship to the NOX2 inhibitor diapocynin (C1), forms π–π interactions with the NOX2 subunit p47phox and exhibits antioxidant properties by inhibiting ROS production in endothelial cells. Targeting the aromatic region of p47phox through π‐interactions is important for inhibiting NOX activity.

Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Martha E. Mac ías Pérez, Maricarmen Hernández Rodríguez, Laura C. Cabrera Pérez, M. Jonathan Fragoso‐Vázquez, José Correa‐Basurto, Itzia I. Padilla‐Martínez, David Méndez Luna, Elvia Mera Jiménez, César Flores Sandoval, Feliciano Tamay Ca Tags: Full Paper Source Type: research