57681-57-9Relevant academic research and scientific papers
Synthesis and structure of alkyl-substituted fused thiophenes containing up to seven rings
He, Mingqian,Zhang, Feixia
, p. 442 - 451 (2007)
We have established a series of synthetic methods to synthesize alkyl-substituted fused thiophenes with degrees of fusion from two to seven rings. These fused thiophene ring compounds have very good solubility in common organic solvents, making possible the solution processing of these compounds for electronic applications. The UV absorption of these fused thiophenes is blue-shifted when compared with their hydrocarbon counterparts. The larger band gaps result in much better stability. Single-crystal X-ray results for 3,6-didecanyldithieno[2,3-d:2′,3′-d′]thieno[3,2-b:4, 5-b″]dithiophene (FT5) and 3,7-didecanylthieno-[3,2-b]thieno[2′, 3′:4,5]thieno[2,3-d]thiophene (FT4) demonstrate that both compounds form π-stacking structures instead of a herringbone-type of packing motif. This more favorable π-stacked structure may lead to better material electronic properties such as mobility in devices fabricated with these compounds.
NOVEL COMPOUNDS HAVING INHIBITORY ACTIVITY ON PROSTAGLANDIN E2 RECEPTOR AND USES THEREOF
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Paragraph 392-395, (2022/03/07)
The present application relates to a novel compound having inhibitory activity on prostaglandin E2 receptor and uses thereof, and provides a compound represented by formula I, a solvate, stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a method of using the same.
Pyrazoles: 'one-pot' synthesis from arenes and carboxylic acids
Gong, Ming,Kim, Jung Keun,Kovalev, Vladimir V.,Kovaleva, Olga V.,Shokova, Elvira A.,Tafeenko, Viktor A.,Wu, Yangjie
supporting information, p. 5625 - 5638 (2020/08/21)
A rapid and efficient method for 'one-pot' synthesis of pyrazoles from (hetero)arenes and carboxylic acids via successive formation of ketones and β-diketones followed by heterocyclization with hydrazine has been developed. The utility of the RCOOH/TfOH/TFAA acylation system for intermediate production of ketones and 1,3-diketones is a key feature of this approach. The preliminary evaluation of the anticancer activity of the synthesized pyrazoles is performed.
Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists
Deng, Huayun,Hu, Jieyu,Hu, Haibei,He, Mingqian,Fang, Ye
scheme or table, p. 4148 - 4152 (2012/07/03)
The optimization of a series of thieno[3,2-b]thiophene-2-carboxylic acid derivatives for agonist activity against the GPR35 is reported. Compounds were optimized to achieve β-arrestin-biased agonism for developing probe molecules that may be useful for elucidating the biology and physiology of GPR35. Compound 13 was identified to the most potent GPR35 agonist, and compounds 30 and 36 exhibited the highest efficacy to cause β-arrestin translocation.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF PATHOLOGICAL CONDITION(S) RELATED TO GPR35 AND/OR GPR35-HERG COMPLEX
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Page/Page column 56, (2012/02/03)
Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject. The compounds having a formula (I), (II) or (III):
Discovery of 2-(4-Methylfuran-2(5 H)-ylidene)malononitrile and thieno[3,2-b ]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists
Deng, Huayun,Hu, Haibei,He, Mingqian,Hu, Jieyu,Niu, Weijun,Ferrie, Ann M.,Fang, Ye
experimental part, p. 7385 - 7396 (2011/12/04)
Screening with dynamic mass redistribution (DMR) assays in a native cell line HT-29 led to identification of two novel series of chemical compounds, 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2- carboxylic acid derivatives, as GPR35 agonists. Of these, 2-(3-cyano-5-(3,4- dichlorophenyl)-4,5-dimethylfuran-2(5H)-ylidene)malononitrile (YE120) and 6-bromo-3-methylthieno[3,2-b]thiophene-2-carboxylic acid (YE210) were found to be the two most potent GPR35 agonists with an EC50 of 32.5 ±1.7 nM and 63.7 ±4.1 nM, respectively. Both agonists exhibited better potency than that of zaprinast, a known GPR35 agonist. DMR antagonist assays, knockdown of GPR35 with interference RNA, receptor internalization assays, and Tango β-arrestin translocation assays confirmed that the agonist activity of these ligands is specific to GPR35. The present study provides novel chemical series as a starting point for further investigations of GPR35 biology and pharmacology.
