1228660-48-7Relevant academic research and scientific papers
Identification of a novel class of autotaxin inhibitors through cross-screening
Castagna, Diana,Duffy, Emma L.,Semaan, Dima,Young, Louise C.,Pritchard, John M.,Macdonald, Simon J. F.,Budd, David C.,Jamieson, Craig,Watson, Allan J. B.
, p. 1149 - 1155 (2015/06/25)
Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists le
Discovery and optimization of 1-(4-(Pyridin-2-yl)benzyl)imidazolidine-2,4- dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists
Van Der Stelt, Mario,Cals, Jos,Broeders-Josten, Silvia,Cottney, Jean,Van Der Doelen, Antoon A.,Hermkens, Marcel,De Kimpe, Vera,King, Angela,Klomp, Jan,Oosterom, Julia,Pols-De Rooij, Ilse,De Roos, Jeroen,Van Tilborg, Martin,Boyce, Susan,Baker, James
, p. 7350 - 7362 (2011/12/04)
Here, we report the identification and optimization of 1-(4-(pyridin-2-yl) benzyl)imidazolidine-2,4-dione derivatives as a novel chemotype with selective cannabinoid CB2 receptor agonist activity. 1 is a potent and selective cannabinoid CB2 receptor agonist (hCB2 pEC50 = 8.6). The compound was found to be metabolically unstable, which resulted in low oral bioavailability in rat (Fpo = 4%) and possessed off-target activity at the hERG ion channel (pKi = 5.5). Systematic modification of physicochemical properties, such as lipophilicity and basicity, was used to optimize the pharmacokinetic profile and hERG affinity of this novel class of cannabinoid CB2 receptor agonists. This led to the identification of 44 as a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist (hCB2 pEC50 = 8.0; hERG pKi po = 100%), which was active in a rat spinal nerve ligation model of neuropathic pain.
1-(4-(PYRIDIN-2-YL)BENZYL)IMIDAZOLIDINE-2,4-DIONE DERIVATIVES
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Page/Page column 8, (2010/06/19)
The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycar
