6280-89-3Relevant articles and documents
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor
Granchi, Carlotta,Lapillo, Margherita,Glasmacher, Sandra,Bononi, Giulia,Licari, Cristina,Poli, Giulio,El Boustani, Maguie,Caligiuri, Isabella,Rizzolio, Flavio,Gertsch, Jürg,Macchia, Marco,Minutolo, Filippo,Tuccinardi, Tiziano,Chicca, Andrea
, p. 1932 - 1958 (2019/02/26)
Monoacylglycerol lipase (MAGL) is the enzyme degrading the endocannabinoid 2-arachidonoylglycerol, and it is involved in several physiological and pathological processes. The therapeutic potential of MAGL is linked to several diseases, including cancer. The development of MAGL inhibitors has been greatly limited by the side effects associated with the prolonged MAGL inactivation. Importantly, it could be preferable to use reversible MAGL inhibitors in vivo, but nowadays only few reversible compounds have been developed. In the present study, structural optimization of a previously developed class of MAGL inhibitors led to the identification of compound 23, which proved to be a very potent reversible MAGL inhibitor (IC50 = 80 nM), selective for MAGL over the other main components of the endocannabinoid system, endowed of a promising antiproliferative activity in a series of cancer cell lines and able to block MAGL both in cell-based as well as in vivo assays.
Cubyl amides: Novel P2X7 receptor antagonists
Gunosewoyo, Hendra,Guo, Jun Liu,Bennett, Maxwell R.,Coster, Mark J.,Kassiou, Michael
supporting information; experimental part, p. 3720 - 3723 (2009/04/06)
Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.
Discovery of potent and selective adamantane-based small-molecule P2X 7 receptor antagonists/interleukin-1β inhibitors
Furber, Mark,Alcaraz, Lilian,Bent, Janice E.,Beyerbach, Armin,Bowers, Keith,Braddock, Martin,Caffrey, Moya V.,Cladingboel, David,Collington, John,Donald, David K.,Fagura, Malbinder,Ince, Frank,Kinchin, Elizabeth C.,Laurent, Celine,Lawson, Mandy,Luker, Timothy J.,Mortimore, Michael M. P.,Pimm, Austen D.,Riley, Robert J.,Roberts, Nicola,Robertson, Mark,Theaker, Jill,Thorne, Philip V.,Weaver, Richard,Webborn, Peter,Willis, Paul
, p. 5882 - 5885 (2008/03/30)
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of t
