Pyroglutamide-Based
P2X7 Receptor Antagonists Targeting
Inflammatory Bowel Disease
Posted on 2019-09-26 - 20:46
This report deals
with the design, the synthesis, and the pharmacological
evaluation of pyroglutamide-based P2X7 antagonists. A dozen were shown
to possess improved properties, among which inhibition of YO-PRO-1/TO-PRO-3
uptake and IL1β release upon BzATP activation of the receptor
and dampening signs of DSS-induced colitis on mice, in comparison
with reference antagonist GSK1370319A. Docking study and biological
evaluation of synthesized compounds has highlighted new SAR, and low
toxicity profiles of pyroglutamides herein described are clues for
the finding of a usable h-P2X7 antagonist drug. Such
a drug would raise the hope for a cure to many P2X7-dependent pathologies,
including inflammatory, neurological, and immune diseases.
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Homerin, Germain; Jawhara, Samir; Dezitter, Xavier; Baudelet, Davy; Dufrénoy, Pierrick; Rigo, Benoît; et al. (2019). Pyroglutamide-Based
P2X7 Receptor Antagonists Targeting
Inflammatory Bowel Disease. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.9b00584
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AUTHORS (22)
GH
Germain Homerin
SJ
Samir Jawhara
XD
Xavier Dezitter
DB
Davy Baudelet
PD
Pierrick Dufrénoy
BR
Benoît Rigo
RM
Régis Millet
CF
Christophe Furman
GR
Guillaume Ragé
EL
Emmanuelle Lipka
AF
Amaury Farce
NR
Nicolas Renault
BS
Boualem Sendid
RC
Rogatien Charlet
JL
Jordan Leroy
MP
Mélodie Phanithavong
CR
Camille Richeval
JW
Jean-François Wiart
DA
Delphine Allorge
SA
Sahil Adriouch