Discovery of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

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Mucroniferanines A-G, Isoquinoline Alkaloids from Corydalis mucronifera

Five pairs of isoquinoline alkaloid enantiomers, mucroniferanines A-E (1-5), two inseparable epimeric pairs, mucroniferanines F and G (6, 7), and 10 known isoquinoline alkaloids (8-17) were obtained from Corydalis mucronifera. The structures were characterized using spectroscopic data analysis, and the absolute configurations were established by ECD and X-ray data analysis. The new compounds except for 3 possess a rare 9-methyl group in the isoquinoline alkaloids, and compounds 2 and 3 possess rare benzo[1,2-d:3,4-d]bis[1,3]dioxole moieties. It is the first report of stereoisomerism involving the 9-methyl phthalideisoquinoline alkaloids. Compounds (-)-4, 6, and 7 exhibited acetylcholinesterase inhibitory activities with IC50 values of 28.3, 12.2, and 11.3 muM, respectively.

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Awesome and Easy Science Experiments about 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

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Protopine alkaloids in horse urine

Protopine was extracted from Fumaria officinalis and purified by column chromatography. Urine samples were collected from horses and a human volunteer that had been administered either F. officinalis or protopine free base. Plant and urine samples were acetylated and analysed by GCMS after solid-phase extraction (SPE). The urinary metabolites of protopine were identified as 4,6,7,13-tetrahydro-9,10-dihydroxy-5-methyl-benzo[e]-l,3-benzodioxolo [4,5-1][2] benzazecin-12(5H)-one, 4,6,7,13-tetrahydro-10-hydroxy-9-methoxy-5-methyl- benzo[e]-1,3-benzodioxolo[4,5-1][2] benzazecin-12(5H)-one and 4,6,7,13-tetrahydro-9-hydroxy-10-methoxy-5-methyl-benzo[e]-1,3-benzodioxolo[4, 5-l][2] benzazecin-12(5H)-one, chelianthifoline, isochelianthifoline and 2-O-desmethylchelianthifoline. The metabolic formation of the tetrahydroprotoberberines by closure of the bridge across N5 and C13 is rate limited and protopine-like metabolites accumulate only when the route is overloaded. Metabolism was qualitatively similar in the horse and human.

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A new application about 3,4-Dibromo-1H-pyrrole-2,5-dione

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Reversible Regulation of Thermoresponsive Property of Dithiomaleimide-Containing Copolymers via Sequential Thiol Exchange Reactions

The facile and efficient functionalization of thermoresponsive polymers based on sequential, reversible thiol-exchange reactions is reported. Well-defined dithiomaleimide-containing polymers have been synthesized via Cu(0)-mediated SET-LRP and characterized by 1H NMR and size exclusion chromatography (SEC). The resulting thermosensitive copolymers were subsequently reacted with various thiols to demonstrate the applicability of the strategy, and the thiol-exchange reaction was found to be very fast and efficient. The cloud point of the prepared copolymers can be continually and reversibly tuned, and desirable functionality can be dynamically exchanged upon sequential addition of functional thiol reagents. Through the substitution by thioglucose, an ON-to-OFF switch for fluorescence of the copolymers along with the generation of a glycopolymer was achieved.

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Simple exploration of 1081-17-0

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Confirming therapeutic target of protopine using immobilized beta2-adrenoceptor coupled with site-directed molecular docking and the target-drug interaction by frontal analysis and injection amount?dependent method

Drug-protein interaction analysis is pregnant in designing new leads during drug discovery. We prepared the stationary phase containing immobilized beta2-adrenoceptor (beta2-AR) by linkage of the receptor on macroporous silica gel surface through N,N?-carbonyldiimidazole method. The stationary phase was applied in identifying antiasthmatic target of protopine guided by the prediction of site-directed molecular docking. Subsequent application of immobilized beta2-AR in exploring the binding of protopine to the receptor was realized by frontal analysis and injection amount?dependent method. The association constants of protopine to beta2-AR by the 2 methods were (1.00?¡À?0.06)?¡Á?105M?1 and (1.52?¡À?0.14)?¡Á?104M?1. The numbers of binding sites were (1.23?¡À?0.07)?¡Á?10?7M and (9.09?¡À?0.06)?¡Á?10?7M, respectively. These results indicated that beta2-AR is the specific target for therapeutic action of protopine in vivo. The target-drug binding occurred on Ser169 in crystal structure of the receptor. Compared with frontal analysis, injection amount?dependent method is advantageous to drug saving, improvement of sampling efficiency, and performing speed. It has grave potential in high-throughput drug-receptor interaction analysis.

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Extended knowledge of 1,1′-(Butane-1,4-diyl)bis(1H-pyrrole-2,5-dione)

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A New Class of Bradykinin Antagonists: Synthesis and in Vitro Activity of Bissuccinimidoalkane Peptide Dimers

A systematic study on the dimerization of the bradykinin (BK) antagonist D-Arg0-Arg1-Pro2-Hyp3-Gly4-Phe5-Ser6-D-Phe7-Leu8-Arg9 has been performed.The first part of this study involved compounds wherein dimerization was carried out by sequentially replacing each amino acid with cysteine and cross-linking with bismaleimidohexane.The second part of this study utilized a series of bissuccinimidoalkane dimers wherein the intervening methylene chain was varied systematically from n = 2 to n = 12 while the point of dimerization was held constant at position 6.The biological activities of these dimers were then evaluated on BK-induced smooth muscle contraction in two different isolated tissue preparations: guinea pig ileum (GPI) and rat uterus (RU).Several of the dimeric BK antagonists displayed remarkable activites and long durations of action.In addition, dimerization at position 4, 7, 8, or 9 produced dimeric analogues with markedly reduced potency.Rank order of antagonist potency as a function of dimerization position is as follows: rat uterus, 6 > 5 > 0 > 2 > 1 >3 >> 4, 7, 8, 9; guinea pig ileum, 6 > 5 > 3 > 2 > 1 > 0 >> 4, 7, 8, 9.Evaluation of the linker length as represented by the number of methylene units indicated an optimal distance between the two monomeric peptides of six to eight methylene moieties.These studies also revealed that the carbon-chain length significantly affected the duration of action in vitro and resulted in partial agonism effects when n > 8.The optimum activity in vitro was achieved with dimerization at position 6 and n = 6 (designated herein as compound 25; alternatively, CP-0127).Similar effects in potency were also seen when the monomeric antagonist D-Arg0-Arg1-Pro2-Hyp3-Gly4-Phe5-Ser6-D-Phe7-Phe8-Arg9 (NPC-567) was dimerized using similar chemistry.These results suggest that the development of BK antagonists of significant therapeutic potential may be possible using a dimerization strategy that can overcome the heretofore limiting problems of potency and in vivo duration of action found with many of the BK antagonists in the literature.

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More research is needed about 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 17057-04-4, in my other articles.

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 17057-04-4, Name is 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid, molecular formula is C11H7NO4

Synthesis and properties of phosphorus containing copoly(bismaleimide)

In this article, a phosphorus containing bismaleimide (V) based on 2- (6-oxido-6H-dibenz <1,2>6-yl)-1,4-dihydroxy phenylene (I) was synthesized and copolymerized with 4,4′-bismaleimidodiphenylmethane (BMDM) in various weight ratio (0-33 phr). DSC scans show that the introduction of V into BMDM has increased the processing window for the resulted copoly(bismaleimide). DMA scans show these cured BMIs exhibit good modulus (~ 2 GPa) up to 400C. There is no tangent peak for these cured BMIs implying that there is no relaxation below 400C. TMA scans show introduction of V into BMDM increase the coefficient of thermal expansion (CTE). However, CTE of these cured BMIs are less than 50 ppm, which is much less than common epoxy. There is no second transition during TMA heating scans up to 440C, so T(g)s of these cured BMIs are higher than 440C, which is consistent with the DMA measurement. TGA heating scans also indicate that they have high thermal stability and their char yields increase with the content of V. Char yields at 800C shift from 48 to 63 in nitrogen and from 0 to 18 in air when 25 phr of V was introduced into BMDM. TGA isothermal experiments show that these cured BMIs are thermally more stable in air than in nitrogen below 450C. Char yields also increase with the content of V. In this article, a phosphorus containing bismaleimide (V) based on 2-(6-oxido-6H-dibenz ?c,e? ?1,2?6-yl)-1,4-dihydroxy phenylene (I) was synthesized and copolymerized with 4,4?-bismaleimidodiphenylmethane (BMDM) in various weight ratio (0-33 phr). DSC scans show that the introduction of V into BMDM has increased the processing window for the resulted copoly(bismaleimide). DMA scans show these cured BMIs exhibit good modulus (approx. 2 GPa) up to 400C. There is no tangent peak for these cured BMIs implying that there is no relaxation below 400C. TMA scans show introduction of V into BMDM increase the coefficient of thermal expansion (CTE). However, CTE of these cured BMIs are less than 50 ppm, which is much less than common epoxy. There is no second transition during TMA heating scans up to 440C, so Tgs of these cured BMIs are higher than 440C, which is consistent with the DMA measurement. TGA heating scans also indicate that they have high thermal stability and their char yields increase with the content of V. Char yields at 800C shift from 48 to 63 in nitrogen and from 0 to 18 in air when 25 phr of V was introduced into BMDM. TGA isothermal experiments show that these cured BMIs are thermally more stable in air than in nitrogen below 450C. Char yields also increase with the content of V.

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Archives for Chemistry Experiments of 1081-17-0

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On the synthesis of protopine alkaloids

(Chemical Equation Presented) For the synthesis of protopine alkaloids, we studied a reaction sequence based on a ring enlargement of indeno[2,1-a][3] benzazepines by a singlet oxygen oxygenation, followed by conversion of an amide carbonyl group of the resultant 10-membered keto-lactam to a methylene group, which is the last step for completion of the synthesis. The key substances, indeno[2,1-a][3]benzazepines, were prepared by Bischler-Napieralski cyclization of alkoxy-substituted 1-(2-bromobenzyl)-3-benzazepin-2-ones. Steric effects of the substituents in this synthesis were examined.

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Discovery of 1122-10-7

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Synthesis and cytotoxicity of novel 3-amino-4-indolylmaleimide derivatives

In an attempt to develop potent and selective antitumor agents, a series of novel 3-amino-4- indolylmaleimides were designed and synthesized. The reaction showed high regioselectivity. The structure of compound 7a was determined by an X-ray single crystal diffraction method. The cytotoxicities of the title compounds were evaluated against HeLa, SMMC 7721 and HL 60 cancer cell lines by a standard MTT assay in vitro. The pharmacological results showed that some of the title compounds displayed moderate or high cytotoxic activity against the tested cell lines. Compound 7d was the most promising compound against the tested cancer cell lines. Structure-activity relationships are discussed based on the experimental data obtained. A hydroxyethylamino group at the 3-position in the side chain of indolylmaleimide is associated with an increase in cytotoxicity. Copyright

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Brief introduction of 1122-10-7

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Maleimide derivative and preparation method and application thereof (by machine translation)

The invention discloses a maleimide derivative and a preparation method thereof as well as. a structural general formula of the maleimide derivative as shown in a formula: I shown in the specification. In-flight vehicle, R1 Sum-up table R2 At least one of the 6 substituted 30 aromatic heterocyclic groups, each, 6 independently 30 selected from the group consisting, 6 of 30 an arylamine group having an arylamine, 5 group 50 of from one or more carbon atoms and an aryl group having ;R an aryl group having an aryl group in an arylamine group of from one to four carbon atoms and an aromatic heterocyclic group is independently selected from the group consisting of an arylamine group, an aryl group, and an aryl group. 3 The maleimide- 1 based 20 derivative of the present invention, 6 incorporates 30 a plurality of electron- 6 rich 30 groups and the highest occupied- 5 orbital 50 level and the lowest-empty-track energy level of at. least one selected from the group consisting of a hydrogen atom, an, alkyl group, an aryl group having an electron, donating ability, and an aromatic heterocyclic group. (by machine translation)

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Extracurricular laboratory:new discovery of 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 17057-04-4 is helpful to your research. Application of 17057-04-4

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Application of maleimide modified graphene quantum dots and porphyrin fluorescence resonance energy transfer in the design of ??turn-on?? fluorescence sensors for biothiols

Two novel fluorescent probes were designed to detect the biothiol in foods using the highly efficient Michael addition reaction between maleimide-derived probes and the biothiol. First, maleimide functionalized GQDs (M-GQDs) were synthesized and used for biothiol identification according to the Michael addition principle. The biothiol can be detected in the range of 5 ¡Á 10?9 to 4 ¡Á 10?7 mol/L and the detection limit was 1.69 ¡Á 10?9 mol/L. Then, a fluorescence resonance energy transfer (FRET) system between M-GQDs and tetrakis (4-aminophenyl) porphyrin (TAPP) for biothiol detection was developed. However, the process of FRET was switched off in the presence of biothiols due to the switch of M-GQDs fluorescence emission to the?ON? mode following the Michael addition mechanism. The system could quickly and accurately detect the biothiol with a detection range of 6.7 ¡Á 10?10 to 2 ¡Á 10?7 mol/L and a detection limit of 2.34 ¡Á 10?10 mol/L. Compared to the single detection system, the FRET system had a wider detection range and lower detection limit, and the related biomolecules did not interfere with the quantitative identification of the biothiol. The proposed method was successfully applied for the determination of the biothiol in foods and human blood samples.

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