51638-13-2Relevant academic research and scientific papers
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes
Wang, Congcong,Zhang, Yu-Fang,Guo, Shimeng,Zhao, Quan,Zeng, Yanping,Xie, Zhicheng,Xie, Xin,Lu, Boxun,Hu, Youhong
, p. 941 - 957 (2020/11/30)
GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington's disease (HD), an incurable monogenic neurodegenerative disorder. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure-activity relationship (SAR) study. Further studies showed that Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation.
Copper ferrite nanoparticles catalyzed formation of β-Ketophosphonates via oxyphosphorylation of styrenes with H-phosphonates: A DFT study on UV–vis absorption spectra
Azaryan, Reza,Daneshfar, Maryam,Moghaddam, Firouz Matloubi,Pirat, Jean-Luc
, (2020/04/21)
Typical copper ferrite nanoparticles (CuFe2O4) were used as a catalyst for one-pot synthesis of β-ketophosphonates via the reaction of alkenes with H-phosphonates under conventional heating conditions. The catalyst was prepared by using the coprecipitation method and was analyzed by physiochemical techniques. By using this catalyst system, several types of useful and new β-ketophosphonate products were obtained in very good to excellent yields under optimized reaction conditions in a novel way. Furthermore, the catalyst is recyclable and reusable from the reaction.
Highly Chemo- And Enantioselective Hydrogenation of 2-Substituted-4-oxo-2-alkenoic Acids
Chen, Weiping,Jiang, Ru,Liu, Xian,Nie, Huifang,Wen, Jialin,Yao, Lin,Zhang, Xumu
supporting information, (2020/07/02)
The highly chemo- and enantioselective hydrogenation of (E)-2-substituted-4-oxo-2-alkenoic acids was established for the first time using the Rh/JosiPhos complex, affording a series of chiral α-substituted-γ-keto acids with excellent results (up to 99% yield and >99% ee) and high efficiency (up to 3000 TON). In addition, the importance of this methodology was further demonstrated by a concise and gram-scale synthesis of the anti-inflammatory drug (R)-flobufen.
Access to chiral α-substituted-β-hydroxy arylphosphonates enabled by biocatalytic dynamic reductive kinetic resolution
Chen, Fener,Huang, Zedu,Li, Zihan,Tao, Yuan,Wang, Zexu,Wu, Xiaofan,Yu, Xiaomin,Zeng, Yiping
supporting information, p. 2672 - 2677 (2020/04/17)
Ketoreductase (KRED)-catalyzed dynamic reductive kinetic resolution (DYRKR) of α-substituted-β-keto arylphosphonates was developed as a generic and stereoselective approach to synthesize chiral α-substituted-β-hydroxy arylphosphonates, with moderate-to-excellent isolated yield (up to 96%), good-to-excellent diastereoselectivity (up to >99 : 99% ee) being achieved.
Solvent-controlled direct radical oxyphosphorylation of styrenes mediated by Manganese(III)
Zhang, Guo-Yu,Li, Cheng-Kun,Li, Da-Peng,Zeng, Run-Sheng,Shoberu, Adedamola,Zou, Jian-Ping
, p. 2972 - 2978 (2016/05/19)
Direct radical oxyphosphorylation of styrenes with diarylphosphine oxides and dialkyl phosphites mediated by Mn(OAc)3 is described. The solvent played a key role in this selective difunctionalization reaction.
Diastereo- and enantioselective asymmetric hydrogenation of α-amido-β-keto phosphonates via dynamic kinetic resolution
Tao, Xiaoming,Li, Wanfang,Li, Xiaoming,Xie, Xiaomin,Zhang, Zhaoguo
supporting information, p. 72 - 75 (2013/03/28)
Dynamic kinetic resolution of various α-amido-β-keto phosphonates via asymmetric hydrogenation proceeded efficiently to give the corresponding β-hydroxy-α-amido phosphonates in high diastereo- and enantioselectivities (up to 99:1 syn/anti, 99.8% ee). The addition of catalytic amounts of CeCl3 3 7H2O is necessary to achieve both good selectivity and catalytic efficiency under mild reaction conditions.
A practical preparation of aryl β-ketophosphonates
Milburn, Robert R.,McRae, Ken,Chan, Johann,Tedrow, Jason,Larsen, Robert,Faul, Margaret
supporting information; experimental part, p. 870 - 872 (2009/05/27)
The condensation of alkyl phosphonates with aryl esters to give β-ketophosphonates may be carried out at elevated temperatures mediated by LiHMDS under Barbier type conditions. The reaction is scalable, does not require specialized cryogenic equipment, and is general for all aryl and heteroaryl esters examined.
Anthelmintic activity of some 3-substituted phenyl-1-alkyl or phenyl propenones and propenamides
Walchshofer,Minjat,Petavy Paris
, p. 1068 - 1071 (2007/10/02)
In a search for new anthelmintic compounds, α,β-unsaturated ketones and amides were synthetized. Their anthelmintic activity was tested against two gastrointestinal worms, a nematode Syphacia obvelata and a cestode Hymenolepis nana. Structure-activity rel
2,5,6,7-tetranor-4,8-inter-m-phenylene PGI2 derivatives
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, (2008/06/13)
Disclosed herein are novel prostaglandin I2 (PGI2) derivatives exhibiting excellent in vivo duration and activities, said derivatives being represented by the general formula: STR1 wherein R1, X, R2 and R3 are as defined herein.
