16728-02-2Relevant articles and documents
Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones
Meza-Avi?a, Maria Elena,Lingerfelt, Mary A.,Console-Bram, Linda M.,Gamage, Thomas F.,Sharir, Haleli,Gettys, Kristen E.,Hurst, Dow P.,Kotsikorou, Evangelia,Shore, Derek M.,Caron, Marc G.,Rao, Narasinga,Barak, Larry S.,Abood, Mary E.,Reggio, Patricia H.,Croatt, Mitchell P.
, p. 1827 - 1830 (2016)
A series of 1,3,4-oxadiazol-2-ones was synthesized and tested for activity as antagonists at GPR55 in cellular beta-arrestin redistribution assays. The synthesis was designed to be modular in nature so that a sufficient number of analogues could be rapidly accessed to explore initial structure–activity relationships. The design of analogues was guided by the docking of potential compounds into a model of the inactive form of GPR55. The results of the assays were used to learn more about the binding pocket of GPR55. With this oxadiazolone scaffold, it was determined that modification of the aryl group adjacent to the oxadiazolone ring was often detrimental and that the distal cyclopropane was beneficial for activity. These results will guide further exploration of this receptor.
Palladium-Catalyzed Carbon Isotope Exchange on Aliphatic and Benzoic Acid Chlorides
Gauthier, Donald R.,Rivera, Nelo R.,Yang, Haifeng,Schultz, Danielle M.,Shultz, C. Scott
supporting information, p. 15596 - 15600 (2018/11/23)
An operationally simple protocol for a palladium-catalyzed 13CO and 14CO exchange with activated aliphatic and benzoic carbonyls is presented. Several 13C and 14C building blocks, natural product derivatives, an
AZACYCLIC COMPOUNDS
-
Paragraph 0652, (2015/11/09)
Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
