150667-24-6Relevant academic research and scientific papers
Fluorescent polarity probes for identifying bovine serum albumin: Amplification effect of para-substituted benzene
Bai, Hongyan,Qian, Junhong,Tian, Haiyu,Pan, Wenwen,Zhang, Lingyi,Zhang, Weibing
, p. 1 - 8 (2014)
Fluorescent probes 1-3 with coumarin as the fluorophore were designed and synthesized for the determination of bovine serum albumin (BSA). All three probes exhibited evidently solvatochromic UV-vis and fluorescence spectra. Compound 3 was the most effective towards the solvent's polarity: 155 nm (vs. 60 nm for 1 and 100 nm for 2) red shift in the emission maximum was found as the solvent changing from cyclohexane to phosphate buffer solution. These compounds were applied to detect BSA based on the hypothesis that the polarity of the microenvironment surrounding the probe will undergo significant change when the probe moves from the bulk solution to the hydrophobic domains of BSA. 3 was the most sensitive towards BSA and the detection limit of BSA was 0.6 μg/mL with 3 as the probe, which ensured the detection of BSA content in fetal bovine serum with good recovery.
4′-Acetamidochalcone derivatives as potential antinociceptive agents
De Campos-Buzzi, Fatima,Padaratz, Pamela,Meira, Aleandra Vergilina,Correa, Rogerio,Nunes, Ricardo Jose,Cechinel-Filho, Valdir
, p. 896 - 906 (2007)
Nine acetamidochalcones were synthesized and evaluated as antinociceptive agents using the mice writhing test. Given intraperitoneally all the compounds were more effective than the two reference analgesic drugs (acetylsalicylic acid and acetaminophen) used for comparison. N-{4-[(2E)-3-(4-nitrophenyl)prop-2- enoyl]phenyl}acetamide (6) was the most effective compound and was therefore selected for more detailed studies. It caused dose-related inhibition in the writhing test, being about 32 to 34-fold more potent than the standard drugs. It was also effective in the second phase of the formalin test and the capsaicin test. These acetamidochalcones, especially compound 6, might be further used as models to obtain new and more potent analgesic drugs.
Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors
Yurttas, Leyla,Kaplancikli, Zafer Asim,Oezkay, Yusuf
, p. 1040 - 1047 (2013)
In this study, some new 2-(4-substituted piperazine-1-yl)-N-[4-(2- methylthiazol-4-yl)phenyl]acetamide derivatives were synthesized. The synthesized compounds were screened for their anticholinesterase activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro Ellman's method. The structural elucidation of the compounds was performed by using IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses results. Biological assays revealed that at 0.1 μM concentration, the most active compounds against AChE were 5n, 5o and 5p that indicated 96.44, 99.83 and 89.70% inhibition rates, respectively. Besides, IC50 value of the compound 5o was determined as 0.011 μM, whereas IC50 value of standard drug donepezil was 0.054 μM. The synthesized compounds did not show any notable inhibitory activity against BChE.
Synthesis, anticandidal activity, and cytotoxicity of some thiazole derivatives with dithiocarbamate side chains
Yurtta, Leyla,?zkay, Yusuf,?ztürk, ?mer,Kaplancikli, Zafer Asim,Demirci, Fatih,G?ger, Gamze,Ulusoylar Yildirim, afak,Abu Mohsen, Usama
, p. 815 - 824 (2014)
Some thiazole derivatives bearing dithiocarbamic acid esters were synthesized in order to investigate their anticandidal activity and cytotoxicity. The structures of the obtained final compounds (6a-j) were confirmed by spectral data (IR, 1H NMR, 13C NMR, and MS) and elemental analysis. The anticandidal activity of the compounds was determined (6a-j) using the microbroth dilution method and their cytotoxicity was evaluated according to the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against normal cells. Contrary to expectations, weak antifungal activity was observed with IC50values ranging between 30 and 403 μg/mL.
Preparation method of acetamide compound
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Paragraph 0035-0047, (2021/05/19)
The invention discloses a preparation method of an acetamide compound, the preparation method comprises the following steps: reacting tetracarbonyl dichloride rhodium, 1, 3-bis (diphenylphosphine) propane, tungsten carbonyl, sodium phosphate, sodium iodide, water, a nitro compound and dimethyl carbonate at 120 DEG C for 24 hours, and after the reaction is completed, performing post-treatment to obtain the acetamide compound. According to the preparation method, dimethyl carbonate serves as a C1 source and also serves as a green solvent, operation is easy, reaction starting raw materials are low in price and easy to obtain, the tolerance range of substrate functional groups is wide, and reaction efficiency is high. Various acetamide compounds can be synthesized according to actual needs, so that the practicability of the method is widened while the operation is convenient.
Chlorination Reaction of Aromatic Compounds and Unsaturated Carbon-Carbon Bonds with Chlorine on Demand
Liu, Feng,Wu, Na,Cheng, Xu
supporting information, p. 3015 - 3020 (2021/05/05)
Chlorination with chlorine is straightforward, highly reactive, and versatile, but it has significant limitations. In this Letter, we introduce a protocol that could combine the efficiency of electrochemical transformation and the high reactivity of chlorine. By utilizing Cl3CCN as the chloride source, donating up to all three chloride atom, the reaction could generate and consume the chlorine in situ on demand to achieve the chlorination of aromatic compounds and electrodeficient alkenes.
Z-Selective Fluoroalkenylation of (Hetero)Aromatic Systems by Iodonium Reagents in Palladium-Catalyzed Directed C?H Activation
Bényei, Attila,Domján, Attila,Egyed, Orsolya,Gonda, Zsombor,Novák, Zoltán,Sályi, Gerg?,Tóth, Balázs L.
supporting information, (2021/11/09)
The direct and catalytic incorporation of fluorine containing molecular motifs into organic compounds resulting high-value added chemicals represents a rapidly evolving part of synthetic methodologies, thus this area is in the focus of pharmaceutical and agrochemical research. Herein we report a stereoselective procedure for direct fluorovinylation of aromatic and heteroaromatic scaffolds. This methodology development has been realized by palladium-catalyzed ortho C?H activation reaction of aniline derivatives featuring the regioselectivity via directing groups such as secondary of tertiary amides, ureas or ketones. The application of non-symmetrical aryl(fluoroalkenyl)-iodonium salts as fluoroalkenylating agents allowed mild reaction conditions in general for this transformation. The scope and limitations have been thoroughly investigated and the feasibility has been demonstrated by more than 50 examples.
Direct Superacid-Promoted Difluoroethylation of Aromatics
Artault, Maxime,Martin-Mingot, Agnès,Thibaudeau, Sébastien,Vitse, Kassandra
supporting information, (2021/12/22)
Under superacid conditions, aromatic amines are directly and regioselectively 1,1-difluoroethylated. Low temperature in situ NMR studies confirmed the presence of benzylic α-fluoronium and α-chloronium ions as key intermediates in the reaction. This method has a wide substrate scope and can be applied to the late-stage functionalization of natural alkaloids and active pharmaceutical ingredients.
Catalyst-free generation of acyl radicals induced by visible light in water to construct C-N bonds
Ran, Maogang,He, Jiaxin,Yan, Boyu,Liu, Wenbo,Li, Yi,Fu, Yunfen,Li, Chao-Jun,Yao, Qiuli
supporting information, p. 1970 - 1975 (2021/03/16)
We describe herein a catalyst-free and redox-neutral photochemical strategy for the direct generation of acyl radicals from α-diketones, and its selective conversion of nitrosoarenes to hydroxyamides or amides with AcOH or NaCl as an additive. The reaction was carried out under mild conditions in water with purple LEDs as the light source. A broad scope of substrates was demonstrated. Mechanistic experiments indicate that α-diketones cleave to give acyl radicals, with hydroxyamides being further reduced to amides.
A novel construction of acetamides from rhodium-catalyzed aminocarbonylation of DMC with nitro compounds
Bao, Zhi-Peng,Miao, Ren-Guan,Qi, Xinxin,Wu, Xiao-Feng
supporting information, p. 1955 - 1958 (2021/03/02)
Dimethyl carbonate (DMC), an environment-friendly compound prepared from CO2, shows diverse reactivities. In this communication, an efficient procedure using DMC as both a C1 building block and solvent in the aminocarbonylation reaction with nitro compounds has been developed. W(CO)6acts both a CO source and a reductant here.
