The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Hydroxynicotinic acid, is researched, Molecular C6H5NO3, CAS is 27828-71-3, about Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors, the main research direction is benzoylpiperidine preparation reversible monoacylglycerol lipase inhibitor human antitumor; Benzoylpiperidine derivatives; MAGL; Monoacylglycerol lipase inhibitors.Safety of 5-Hydroxynicotinic acid.
An interesting enzyme of the endocannabinoid system is monoacylglycerol lipase (MAGL). This enzyme, which metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG), has attracted great interest due to its involvement in several physiol. and pathol. processes, such as cancer progression. Exptl. evidences highlighted some drawbacks associated with the use of irreversible MAGL inhibitors in vivo, therefore the research field concerning reversible inhibitors is rapidly growing. In the present manuscript, the class of benzoylpiperidine-based MAGL inhibitors was further expanded and optimized. Enzymic assays identified some compounds in the low nanomolar range and steered mol. dynamics simulations predicted the dissociation itinerary of one of the best compounds from the enzyme, confirming the observed structure-activity relationship. Biol. evaluation, including assays in intact U937 cells and competitive activity-based protein profiling experiments in mouse brain membranes, confirmed the selectivity of the selected compounds for MAGL vs. other components of the endocannabinoid system. Future studies on the potential use of these compounds in the clin. setting are also supported by the inhibition of cell growth observed both in cancer organoids derived from high grade serous ovarian cancer patients and in pancreatic ductal adenocarcinoma primary cells, which showed genetic and histol. features very similar to the primary tumors.
《Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(5-Hydroxynicotinic acid)Safety of 5-Hydroxynicotinic acid.
Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method