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

doi:10.1039/c4md00319e

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

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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. This journal is

Original language	English (US)
Pages (from-to)	75-79
Number of pages	5
Journal	MedChemComm
Volume	6
Issue number	1
DOIs	https://doi.org/10.1039/c4md00319e
State	Published - Jan 1 2015

ASJC Scopus subject areas

Biochemistry
Pharmaceutical Science

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10.1039/c4md00319e

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AU - Chini, Maria Giovanna

AU - Ferroni, Claudia

AU - Cantone, Vincenza

AU - Dambruoso, Paolo

AU - Varchi, Greta

AU - Pepe, Antonella

AU - Fischer, Katrin

AU - Pergola, Carlo

AU - Werz, Oliver

AU - Bruno, Ines

AU - Riccio, Raffaele

AU - Bifulco, Giuseppe

PY - 2015/1/1

Y1 - 2015/1/1

N2 - 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. This journal is

AB - 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. This journal is

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

Abstract

ASJC Scopus subject areas

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