31366-07-1Relevant articles and documents
Identification of a novel neuropeptide s receptor antagonist scaffold based on the sha-68 core
Bool, Heather,Clark, Stewart D.,Gay, Elaine,Jahan, Rajwana,Jewula, Gabriel,McElhinny, Charles,Runyon, Scott,Snyder, Rodney,Uprety, Rajendra,Zarkin, Allison,Zhang, Yanan
, (2021/10/20)
Activation of the neuropeptide S receptor (NPSR) system has been shown to produce an-xiolytic-like actions, arousal, and enhance memory consolidation, whereas blockade of the NPSR has been shown to reduce relapse to substances of abuse and duration of anesthetics. We report here the discovery of a novel core scaffold (+) N-benzyl-3-(2-methylpropyl)-1-oxo-3-phenyl-1H,3H,4H,5H,6H,7H-furo[3,4-c]pyridine-5-carboxamide with potent NPSR antagonist activity in vitro. Pharmacokinetic parameters demonstrate that 14b reaches pharmacologically relevant levels in plasma and the brain following intraperitoneal (i.p.) administration, but is cleared rapidly from plasma. Compound 14b was able to block NPS (0.3 nmol)-stimulated locomotor activity in C57/Bl6 mice at 3 mg/kg (i.p.), indicating potent in vivo activity for the structural class. This suggests that 14b can serve as a useful tool for continued mapping of the pharmacological functions of the NPS receptor system.
Direct C-H Arylation of Aldehydes by Merging Photocatalyzed Hydrogen Atom Transfer with Palladium Catalysis
Chen, Guangying,Cheng, Gui-Juan,Guo, Bin,Li, Xiaobao,Ran, Chongzhao,Wang, Lu,Wang, Ting,Wei, Jun-Jie,Zheng, Caijuan,Zheng, Chao
, p. 7543 - 7551 (2020/08/21)
Herein, we report that merging palladium catalysis with hydrogen atom transfer (HAT) photocatalysis enabled direct arylations and alkenylations of aldehyde C-H bonds, facilitating visible light-catalyzed construction of a variety of ketones. Tetrabutylammonium decatungstate and anthraquinone were found to act as synergistic HAT photocatalysts. Density functional theory calculations suggested a Pd0-PdII-PdIII-PdI-Pd0 pathway and revealed that regeneration of the Pd0 catalyst and the photocatalyst occurs simultaneously in the presence of KHCO3. This regeneration features a low energy barrier, promoting efficient coupling of the palladium catalytic cycle with the photocatalytic cycle. The work reported herein suggests great promise for further applications of HAT photocatalysis in palladium-catalyzed cross-coupling and C-H functionalization reactions to be successful.
Alkaline cage compound, its preparation method and catalyst (by machine translation)
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Paragraph 0087; 0090, (2019/11/04)
The application relates to a alkaline cage compound, its preparation method and catalyst. The application of the alkaline cage compound, containing 6 has a strong alkaline secondary amine group of Soluble in many common organic solvent (such as ethyl acet