78979-61-0Relevant academic research and scientific papers
Rational Design, Synthesis and Evaluation of Oxazolo[4,5-c]-quinolinone Analogs as Novel Interleukin-33 Inhibitors
Byun, Youngjoo,Cho, Haelim,Ho Jeon, Young,Hoon Kim, Kyong,Jang, Geonhee,Kim, Yujin,Lee, Kiho,Lee, Taeyun,Ma, Chao,Paek, Jiwon,Park, Seonghu,Shin -, Yujin,Son, Sang-Hyun,Son, Seyoung,Woo Jung, Yong,Yong Lee, Ki
, p. 3702 - 3712 (2021/11/19)
Interleukin-33 (IL-33) is an epithelial-derived cytokine that plays an important role in immune-mediated diseases such as asthma, atopic dermatitis, and rheumatoid arthritis. Although IL-33 is considered a potential target for the treatment of allergy-rel
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
Lin, Yinuo,Ahmed, Wasim,He, Min,Xiang, Xuwen,Tang, Riyuan,Cui, Zi-Ning
, (2020/10/02)
In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory ac
NOVEL QUINOLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ALLERGIC DISEASES SUCH AS ASTHMA OR ATOPIC DERMATITIS INCLUDING THE QUINOLINONE DERIVATIVE AS ACTIVE INGREDIENT
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Paragraph 0028; 0045-0046; 0050, (2020/05/29)
The present invention relates to anovel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The qu
Radical C-H Arylation of Oxazoles with Aryl Iodides: Dppf as an Electron-Transfer Mediator for Cs2CO3
Guo, Zhengwei,Li, Man,Mou, Xue-Qing,He, Gang,Xue, Xiao-Song,Chen, Gong
supporting information, p. 1684 - 1687 (2018/03/23)
A radical C-H arylation reaction of oxazoles with (hetero)aryl iodides using Cs2CO3 as base/electron donor and 1,1′-bis(diphenylphosphino) ferrocene (dppf) as a catalytic SET mediator is reported. The overall reaction likely follows the general base-promoted homolytic aromatic substitution mechanism through a radical-chain pathway. DFT calculations suggest that dppf forms a complex with CsCO3-, enhancing its SET reducing ability to generate an aryl radical from ArI.
Design, synthesis and biological evaluation of 2,4-disubstituted oxazole derivatives as potential PDE4 inhibitors
Li, Ya-Sheng,Hu, De-Kun,Zhao, Dong-Sheng,Liu, Xing-Yu,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning,Zhang, Lian-Hui
, p. 1852 - 1859 (2017/03/08)
In this study, a series of pyrazole derivatives containing 4-phenyl-2-oxazole moiety were designed and synthesized in a concise way, some of which exhibited considerable inhibitory activity against PDE4B and blockade of LPS-induced TNF-α release. Compound
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors
Senger, Johanna,Melesina, Jelena,Marek, Martin,Romier, Christophe,Oehme, Ina,Witt, Olaf,Sippl, Wolfgang,Jung, Manfred
supporting information, p. 1545 - 1555 (2016/03/08)
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine residues of several non-histone proteins. Here we report the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short synthetic proce
A silver-mediated one-step synthesis of oxazoles
Ritson, Dougal J.,Spiteri, Christian,Moses, John E.
supporting information; experimental part, p. 3519 - 3522 (2011/06/24)
A silver-mediated one-step procedure to 2,4-disubstituted and 2,4,5-trisubstituted oxazoles has been developed. The method is complementary to existing technologies, yet provides advantages with regard to simplicity, efficiency, and performance. The silver product can be readily recycled, thus minimizing waste.
Mechanism selection for regiocontrol in base-assisted, palladium-catalysed direct C-H coupling with halides: First approach for oxazole- and thiazole-4-carboxylates
Théveau, Laure,Verrier, Cécile,Lassalas, Pierrik,Martin, Thibaut,Dupas, Georges,Querolle, Olivier,Van Hijfte, Luc,Marsais, Francis,Hoarau, Christophe
supporting information; experimental part, p. 14450 - 14463 (2012/01/15)
Both base-assisted non-concerted metallation-deprotonation (nCMD) and concerted metallation-deprotonation (CMD) have been identified as two potent operating mechanisms in palladium-catalysed direct C-H coupling of oxazole and thiazole-4-carboxylate esters
Carbonates: Eco-friendly solvents for palladium-catalysed direct arylation of heteroaromatics
Dong, Jia Jia,Roger, Julien,Verrier, Cecile,Martin, Thibaut,Le Goff, Ronan,Hoarau, Christophe,Doucet, Henri
experimental part, p. 2053 - 2063 (2011/02/25)
The palladium-catalysed direct 2-, 4- or 5-arylation of a wide range of heteroaromatics with aryl halides proceed in moderate to good yields using the eco-friendly solvents carbonates. The best yields were obtained using benzoxazole or thiazole derivatives. The arylation of furan, thiophene, pyrrole, imidazole or isoxazole derivatives was found to require a more elevated reaction temperature. The Royal Society of Chemistry 2010.
Palladium-catalyzed carbonylative C-H activation of heteroarenes
Wu, Xiao-Feng,Anbarasan, Pazhamalai,Neumann, Helfried,Beller, Matthias
supporting information; experimental part, p. 7316 - 7319 (2010/11/05)
Not only carbonylation: The first carbonylative cross-coupling reactions towards ketones using C-H activation have been developed. Various heteroarenes, such as oxazoles, thiazoles, and imidazoles were used as coupling partners in this methodology. DBU =
