34035-05-7Relevant academic research and scientific papers
Carbon–Carbon Bond Formation for the Synthesis of 5-Aryl-2-Substituted Furans Catalyzed by K3[Fe(CN)6]
Ambika,Singh, Pradeep Pratap
, (2021/10/05)
An efficient method for the carbon–carbon bond formation at C-5 position of 2-substituted furans to provide a range of π-diverse 5-aryl-2-substituted furan derivatives in 58–80% yield has been reported. The method employs several advantages such as use of catalytic amount of K3[Fe(CN)6] under mild conditions and short reaction time with high yields. Also, a variety of anilines with a variety of functional groups can be employed for the synthesis of 5-aryl-2-substituted furans. Graphic Abstract: [Figure not available: see fulltext.]
5-Aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety as potential PTP1B inhibitors
Niu, Tianwei,Wang, Peipei,Li, Cheng,Dou, Tong,Piao, Huri,Li, Jia,Sun, Liangpeng
, (2020/12/04)
Two series of 5-aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, 5g was found to have the best PTP1B inhibitory potency (IC50 = 2.66 ± 0.16 μM) and the best cell division cycle 25 homolog B (CDC25B) inhibitory potency (IC50 = 0.25 ± 0.02 μM). Enzymatic data together with molecular modeling results demonstrated that the introduction of a sec-butyl group at the 2-position of the carboxyl group remarkably improved the PTP1B inhibitory activity.
Discovery of (5-Phenylfuran-2-yl)Methanamine derivatives as new human sirtuin 2 Inhibitors
Wang, Lijiao,Li, Chao,Chen, Wei,Song, Chen,Zhang, Xing,Yang, Fan,Wang, Chen,Zhang, Yuanyuan,Qian, Shan,Wang, Zhouyu,Yang, Lingling
, (2019/08/07)
Human sirtuin 2 (SIRT2), a member of the sirtuin family, has been considered as a promising drug target in cancer, neurodegenerative diseases, type II diabetes, and bacterial infections. Thus, SIRT2 inhibitors have been involved in effective treatment strategies for related diseases. Using previously established fluorescence-based assays for SIRT2 activity tests, the authors screened their in-house database and identified a compound, 4-(5-((3-(quinolin-5-yl)ureido)methyl) furan-2-yl)benzoic acid (20), which displayed 63 ± 5% and 35 ± 3% inhibition against SIRT2 at 100 μM and 10 μM, respectively. The structure-activity relationship (SAR) analyses of a series of synthesized (5-phenylfuran-2-yl)methanamine derivatives led to the identification of a potent compound 25 with an IC50 value of 2.47 μM, which is more potent than AGK2 (IC50 = 17.75 μM). Meanwhile, 25 likely possesses better water solubility (cLogP = 1.63 and cLogS = ?3.63). Finally, the molecular docking analyses indicated that 25 fitted well with the induced hydrophobic pocket of SIRT2.
Palladium(II)-N-Heterocyclic Carbene Complexes: Efficient Catalysts for the Direct C-H Bond Arylation of Furans with Aryl Halides
Kalo?lu, Murat,?zdemir, ?smail
, (2018/05/03)
This paper contains the synthesis and characterization of the seven new benzimidazolium salts and their corresponding new palladium(II)-NHC complexes with the general formula [PdX2(NHC)2], (NHC?=?N-heterocyclic carbene, X?=?Cl or Br)
Access to Densely Functionalized Chalcone Derivatives with a 2-Pyridone Subunit via Pd/Cu-Catalyzed Oxidative Furan-Yne Cyclization of N -(2-Furanylmethyl) Alkynamides under Air
Yang, Yongjie,Fei, ChengCheng,Wang, Kai,Liu, Bo,Jiang, Dingxin,Yin, Biaolin
supporting information, p. 2273 - 2277 (2018/04/30)
A protocol for synthesis of chalcone derivatives with a 2-pyridone subunit from N-(2-furanylmethyl) alkynamides is reported. This synthesis involves Pd/Cu-catalyzed oxidative furan-yne cyclization at room temperature in air and may proceed via nucleopalladation of the alkyne to form a vinylpalladium intermediate, with a furan ring acting as the nucleophile.
D-3-phosophoglycerate dehydrogenase allosteric inhibitor and application thereof
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Paragraph 0055-0057, (2018/02/04)
The invention discloses a D-3-phosophoglycerate dehydrogenase allosteric inhibitor and an application thereof. The structure of the D-3-phosophoglycerate dehydrogenase allosteric inhibitor is shown in a formula I defined in the specification, wherein R1,
Antibacterial and antifungal properties of guanylhydrazones
Ajda?i?, Vladimir,Lazi?, Jelena,Moji?evi?, Marija,?egan, Sandra,Nikodinovic-Runic, Jasmina,Opsenica, Igor M.
, p. 641 - 649 (2017/08/09)
A series of novel guanylhydrazones were designed, synthesized and characterized. All the compounds were screened for their antibacterial and antifungal activity. Compounds 26 and 27 showed excellent antibacterial activities against Staphylococcus aureus A
Small molecule near-infrared boron dipyrromethene donors for organic tandem solar cells
Li, Tian-Yi,Meyer, Toni,Ma, Zaifei,Benduhn, Johannes,Korner, Christian,Zeika, Olaf,Vandewal, Koen,Leo, Karl
supporting information, p. 13636 - 13639 (2017/11/06)
Three furan fused boron dipyrromethenes (BODIPYs) with a CF3 group on the meso-carbon are synthesized as near-infrared absorbing materials for vacuum processable organic solar cells. The best single junction device reaches a short-circuit curre
A HIGH-THROUGHPUT ASSAY FOR IDENTIFYING SMALL MOLECULES THAT MODULATE AMP-ACTIVATED PROTEIN KINASE (AMPK)
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Page/Page column 61;, (2016/02/29)
The present invention provides an in vitro method for identifying a compound that modulates adenosine monophosphate-activated protein kinase (AMPK) for the manufacture of a diagnostic or therapeutic agent. The present invention further provides an assay for identifying a compound that modulates AMPK.
Design and synthesis of natural product derivatives with selective and improved cytotoxicity based on a sesquiterpene scaffold
Zhang, Yang,Zhang, Zhuowei,Wang, Bo,Liu, Ling,Che, Yongsheng
supporting information, p. 1885 - 1888 (2016/04/05)
Brasilamide E (1) is a bisabolane sesquiterpenoid isolated from the solid-substrate fermentation cultures of a plant endophytic fungus Paraconiothyrium brasiliense. The compound specifically inhibited proliferation of the MCF-7 cells, but did not show cyt
