6-oxopiperidine-2-carboxylate and Inflammatory-Bowel-Diseases

6-oxopiperidine-2-carboxylate has been researched along with Inflammatory-Bowel-Diseases* in 1 studies

Other Studies

1 other study(ies) available for 6-oxopiperidine-2-carboxylate and Inflammatory-Bowel-Diseases

ArticleYear
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
    Journal of medicinal chemistry, 2020, 03-12, Volume: 63, Issue:5

    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

    Topics: Animals; Cell Survival; Dextran Sulfate; Drug Delivery Systems; Female; HEK293 Cells; Humans; Inflammatory Bowel Diseases; Mice; Mice, Inbred C57BL; Purinergic P2X Receptor Antagonists; Receptors, Purinergic P2X7

2020