Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitors†
Maria Giovanna Chini,Claudia Ferroni,Vincenza Cantone,Paolo Dambruoso,Greta Varchi,Antonella Pepe,Katrin Fischer,Carlo Pergola,Oliver Werz,Ines Bruno,Raffaele Riccio,Giuseppe Bifulco
Abstract
We report a new potent revisited version of a triazole-based inhibitor obtained by structure-based drug design on the human mPGES-1 crystal structure. Moreover, we disclosed the substitution with a halogen atom at position 5 as a new key factor influencing the biological activity on the mPGES-1 enzyme.
