104317-95-5Relevant academic research and scientific papers
Discovery of G Protein-Biased Ligands against 5-HT7R
Lee, Jieon,Kwag, Rina,Lee, Soyeon,Kim, Doyoung,Woo, Jiwan,Cho, Yakdol,Kim, Hak Joong,Kim, Jeongjin,Jeon, Byungsun,Choo, Hyunah
, p. 7453 - 7467 (2021)
There has been significant attention concerning the biased agonism of G protein-coupled receptors (GPCRs), and it has resulted in various pharmacological benefits. 5-HT7R belongs to a GPCR, and it is a promising pharmaceutical target for the treatment of neurodevelopmental and neuropsychiatric disorders. Based on our previous research, we synthesized a series of 6-chloro-2′-methoxy biphenyl derivatives 1, 2, and 3 with a variety of amine scaffolds. These compounds were evaluated for their binding affinities to 5-HTR subtypes and their functional selectivity toward the Gs protein and the β-arrestin signaling pathways of 5-HT7R. Among them, 2-(6-chloro-2′-methoxy-[1,1′-biphenyl]-3-yl)-N-ethylethan-1-amine, 2b, was found to be a G-protein-biased ligand of 5-HT7R. In an in vivo study with Shank3 transgenic mice, the self-grooming behavior test was performed with 2b, which increased the duration of self-grooming. The experiments further suggested that 5-HT7R is associated with autism spectrum disorders (ASDs) and could be a therapeutic target for the treatment of stereotypy in ASDs.
Water bridges are essential to neonicotinoids: Insights from synthesis, bioassay and molecular modelling studies
Zhu, Chengchun,Li, Guanglong,Xiao, Keya,Shao, Xusheng,Cheng, Jiagao,Li, Zhong
, p. 255 - 258 (2019)
Water-bridged H-bonds have been observed in many cases of ligand-receptor recognitions. To explore the roles of water bridges in the binding of neonicotinoids with receptors, twenty-four neonicotinoid compounds with nine fragments, including 1H-1,2,3-tria
2-(1,2,3-TRIAZOL-2-YL)BENZAMIDE AND 3-(1,2,3-TRIAZOL-2-YL)PICOLINAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Paragraph 0447; 0448, (2015/06/17)
The present invention relates to 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives of formula (I) wherein Ar1, Q, and R1 to R5 are as described in the description, to their preparation, to
2-(1,2,3-TRIAZOL-2-YL)BENZAMIDE AND 3-(1,2,3-TRIAZOL-2-YL)PICOLINAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 60; 61, (2013/05/23)
The present invention relates to 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2- yl)picolinamide derivatives of formula (I) Formula (I) wherein Ar1, Q, and R1 to R5 are as described in the description, to their pre
Indole derivatives as MCP-1 receptor antagonists
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, (2008/06/13)
A compound of Formula I, wherein: R1 is hydrogen, halo, methyl, ethyl or methoxy; R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is a halo group, lower alkyl, lower alkenyl, lower alkynyl, alkoxy, trifluoromethyl, nitro, cyano, trifluoromethoxy, C(O)R7, or S(O)nR7 where n is 0, 1 or 2 and R7 is an alkyl group; R4 is a halo, trifluoromethyl, methylthio, methoxy, trifluoromethoxy or lower alkyl, lower alkenyl or lower alkynyl or COR8 where R8 is lower alkyl; R6 is hydrogen, halo, lower alkyl, lower alkenyl, lower alkynyl or COR9 where R9 is lower alkyl; provided that when R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy, R5 and R6 are both hydrogen, and one of R3 or R4 is not halo or trifluoromethyl; or a pharmaceutically acceptable salt or prodrug thereof. These compounds have useful activity for the treatment of inflammatory disease, specifically in antagonizing an MCP-1 mediated effect in a warm-blooded animal such as a human being.
PYRAN/DIOXAN DERIVATIVES AND USE THEREOF IN LIQUID CRYSTAL MEDIA
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Page/Page column 56-57, (2010/11/25)
The invention relates to pyran/dioxan derivatives and use thereof as components in liquid crystal media. The invention further relates to liquid crystal and electrooptical display elements, comprising said liquid crystal media.
Indolin-2-one derivatives, preparation and their use as ocytocin receptor ligands
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, (2008/06/13)
The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.
