Homerin, Germain published the artcilePyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease, Synthetic Route of 617-52-7, the publication is Journal of Medicinal Chemistry (2020), 63(5), 2074-2094, database is CAplus and MEDLINE.
This report deals with the design, the synthesis, and the pharmacol. 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 biol. 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, neurol., and immune diseases.
Journal of Medicinal Chemistry published new progress about 617-52-7. 617-52-7 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Aliphatic hydrocarbon chain,Ester, name is Dimethyl itaconate, and the molecular formula is C7H10O4, Synthetic Route of 617-52-7.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics