Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitors. Issue 1 (3rd October 2014)

• Record Type: Journal Article
• Authors: Chini, Maria Giovanna; Ferroni, Claudia; Cantone, Vincenza; Dambruoso, Paolo; Varchi, Greta; Pepe, Antonella; Fischer, Katrin; Pergola, Carlo; Werz, Oliver; Bruno, Ines; Riccio, Raffaele; Bifulco, Giuseppe
• Is Part Of: MedChemComm. Volume 6:Issue 1(2015:Jan.)
• Page Start: 75
• Page End: 79
• Publication Date: 2014-10-03
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c4md00319e
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : Halogen bonding as a new key interaction is useful for the design of novel triazole derivatives as mPGES-1 inhibitors. 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.