Issue 1, 2015

Elucidating new structural features of the triazole scaffold for the development of 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.

Graphical abstract: Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitors

Supplementary files

Article information

Article type
Concise Article
Submitted
22 Jul 2014
Accepted
14 Sep 2014
First published
15 Sep 2014

Med. Chem. Commun., 2015,6, 75-79

Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitors

M. G. Chini, C. Ferroni, V. Cantone, P. Dambruoso, G. Varchi, A. Pepe, K. Fischer, C. Pergola, O. Werz, I. Bruno, R. Riccio and G. Bifulco, Med. Chem. Commun., 2015, 6, 75 DOI: 10.1039/C4MD00319E

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