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ALKALOIDS OF Fumaria parviflora

The total alkaloids of the plant Fumaria parviflora Lam., collected in Ashkhabad Province (Turkmen SSR), in the flowering and incipient fruit-bearing period have been studied.The methanolic extraction of 10.5 kg of the plant yielded 0.39percent of total alkaloids, from which cheilanthifoline, scoulerine, parfumine, norjusiphine, isoboldine, coclaurine, dihydrosanguinarine, stylopine, sanguinarine, oxysanguinarine, adlumine, adlumidine, hydrastine, bicuculline, protopine, cryptopine, adlumidiceine, N-methyladlumine, a base with mp 281-282 deg C, and a new alkaloid – d-fumaricine – have been isolated from the plant for the first time.

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Properties and Exciting Facts About 1122-10-7

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Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor

JAK family kinases are important mediators of immune cell signaling and Janus Kinase 3 (JAK3) has long been indicated as a potential target for autoimmune disorders. Intensive efforts to develop highly selective JAK3 inhibitors have been underway for many years. However, because of JAK3’s strong binding preference to adenosine 5?-triphosphate (ATP), a number of inhibitors exhibit large gaps between enzymatic and cellular potency, which hampers efforts to dissect the roles of JAK3 in cellular settings. Using a targeted covalent inhibitor approach, we discovered compound 32, which overcame ATP competition (1 mM) in the enzymatic assay, and demonstrated significantly improved inhibitory activity for JAK3-dependent signaling in mouse CTLL-2 and human peripheral blood mononuclear cells. Compound 32 also exhibited high selectivity within the JAK family and good pharmacokinetic properties. Thus, it may serve as a highly valuable tool molecule to study the overlapping roles of JAK family kinases in complex biological settings. Our study also suggested that for covalent kinase inhibitors, especially those targeting kinases with low Km ATP values, the reversible interactions between molecules and proteins should be carefully optimized to improve the overall potency.

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Awesome Chemistry Experiments For 1193-54-0

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Synthesis, Properties, and Light Fastness of Diaminomaleimide and Some of its Derivatives

Reaction of ammonia with dichloromaleimide (3) yields the aminomaleimides 1 and 4, 2,3-dichloromaleamide (6), and 2,3-diaminofumaramide (2) depending on solvent, temperature, and pressure.The reactivity of the eneamino groups in 1 and 4 are remarkably different, 1 reacts like an amine while 4 resembles an amide.Interpretation of the ultraviolett and fluorescence spectra shows that 1, 4, and the acyl derivatives 13 – 15 can be classified as meropolar dyes.Light fastness values and fluorescence yields show a reverse correlation by change of solvent.Photochemical decomposition and fluorescence show a reactivity-selectivity correlation by variation of substituents at the double bond.

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

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A new protoberberine alkaloid from Meconopsis simplicifolia (D. Don) Walpers with potent antimalarial activity against a multidrug resistant Plasmodium falciparum strain

Ethnopharmacological relevance The aerial components of Meconopsis simplicifolia (D. Don) Walpers are indicated in Bhutanese traditional medicine for treating malaria, coughs and colds, and the infections of the liver, lung and blood. This study is to validate the ethnopharmacological uses of this plant and also identify potent antimalarial drug leads through bioassays of its crude extracts and phytochemical constituents. Materials and methods Meconopsis simplicifolia (D. Don) Walpers was collected from Bhutan and its crude MeOH extract was subjected to acid-base fractionation. Through repeated extractions, separations and spectroscopic analysis, the alkaloids obtained were identified and tested for their antimalarial and cytotoxicity activities. Results Phytochemical studies resulted in the isolation of one new protoberberine type alkaloid which we named as simplicifolianine and five known alkaloids: protopine, norsanguinarine, dihydrosanguinarine, 6-methoxydihydrosanguinarine and oxysanguinarine. Among the five of the alkaloids tested, simplicifolianine showed the most potent antiplasmodial activities against the Plasmodium falciparum strains, TM4/8.2 (chloroquine-antifolate sensitive strain) and K1CB1 (multidrug resistant strain) with IC50 values of 0.78 mug/mL and 1.29 mug/mL, respectively. The compounds tested did not show any significant cytotoxicity activities against human oral carcinoma KB cells and normal Vero cells of African kidney epithelial cells. Conclusions This study validated the traditional uses of the plant for the treatment of malaria and identified a new alkaloid, simplicifolianine as a potential antimalarial drug lead.

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

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Synthesis of arcyriarubine regioisomers by Pd(0)-catalysis or via lithiated indole derivatives – Conformational analysis by semiempirical and X-ray methods

Regioisomers of arcyriarubines were synthesized by the reaction of N- protected indoles with dibromomaleimide either in the presence of a Pd(0)- catalyst or n-BuLi. Methods for N-alkylation of these bisindolylmaleimides and deprotection of the indole-N are described. The structure of the bisindolylmaleimide 11 was studied by semiempiric quantum-chemical calculations, the structure of its derivative 14b was ascertained by X-ray analysis.

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Rhodium(III)-catalyzed C-H activation/annulation with vinyl esters as an acetylene equivalent

The behavior of electron-rich alkenes in rhodium-catalyzed C-H activation/annulation reactions is investigated. Vinyl acetate emerges as a convenient acetylene equivalent, facilitating the synthesis of sixteen 3,4-unsubstituted isoquinolones, as well as select heteroaryl-fused pyridones. The complementary regiochemical preferences of enol ethers versus enol esters/enamides is discussed.

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The Chemistry of Lactim Ethers. II. Reaction of Lactim Ethers with 2-Carbethoxymethyl Piperidines

Annulation reactions of methyl valerolactim (2) and methyl caprolactim (3) with cyclic beta-aminoesters, such as 2-carbethoxymethyl piperidine derivatives (4 or 5), often gave two kinds of products apparently arising from the imine and enamine forms of 2 and 3.These chemical properties were consistent with NMR observations of lactim ethers in CD3OD solution.Keywords- lactim ethers; 2-carbethoxymethyl piperidines; imine-enamine tautomeric equilibrium; annulation; imine type product; enamine type product

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MALEIMIDE-FURANYL COMPOUNDS THAT CAN BE USED IN A GENERAL METHOD FOR PREPARING MALEIMIDE-OLIGONUCLEOTIDE DERIVATIVES

The compounds of formula (I) substantially in exo form or salts thereof, wherein: X is a biradical selected from ?(CH2)n?*, ?(CH2CH2O)nCH2CH2?*, methylcyclohexyl and methylphenyl; n is an integer ranging between 1 and 30; Y is a radical selected from ?COOH, a substituted phosphoramidite radical and N-hydroxysuccinimide ester (or other active ester) of carboxylic acid; and * represents the place through which X binds to Y, are useful in a general process for solid-phase preparation of maleimide-oligonucleotide derivatives.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 5264-35-7, name is 5-Methoxy-3,4-dihydro-2H-pyrrole, introducing its new discovery. SDS of cas: 5264-35-7

Organic syntheses via transition metal complexes. 96. 1-azacycloalkene and 2-azabicycloalkene derivatives of 4-amino-1-metalla-1,3-dienes by reaction of saturated lactims with (1-alkynyl)carbene complexes of chromium and tungsten

Reaction of five- and six-membered O-alkyl lactims ?(CH2)n-N=C(OR)? 5 (n = 3) and 7 (n = 4) with (1-alkynyl)carbene complexes (CO)5M=C(OEt)C?CPh 1 (a, M = Cr; b, W) gives binuclear 1-alkoxy-2-azabicyclo[n.2.0]alkene derivatives (E)-6 and (E)-8, respectively, in 90-94% yields. Reaction of seven- and eight-membered O-alkyl lactims ?(CH2)n-N=C(OR)? 9 (n = 5) and 11 (n = 6) with compounds 1 affords mononuclear 4-(1-aza-cyclo-2-alken-1-yl) 1-metalla-1,3-butadienes (E)-10 and (E)-11, respectively, but no binuclear derivatives. Both mono- and binuclear metal compounds undergo fast transformations on contact with silica gel. Chromatography of the binuclear tungsten compound (E)-6b on silica gel results in fragmentation of the (cyclobutenyl)carbene unit to give 1,11-bis(tungsta)-5-azaundeca-1,3,6,8,10-pentaene (13) as well as in hydrolysis of the 2-alkoxy pyrrolidine unit with formation of a bis(carbene) derivative 15 of an amino acid. Compound 13, on extended contact with silica gel, undergoes cyclization and subsequent hydrolysis to 2-azabicyclo[3.3.0]octenone 14. Thermal fragmentation of the mononuclear dihydroazepine compound (E)-10c affords dihydro- and tetrahydropyrrolo[1,2-alpha]azepines 17 and 18, respectively. X-ray crystal structural data are reported for the binuclear compound (E)-6b as well as for mononuclear compounds (E)-10c and 14.

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Double-indole maleic imide derivative and its preparation and use (by machine translation)

Provides a double-indole maleic imide derivative and its preparation and use. The double-indole maleic imide derivatives have good alpha – glucosidase inhibiting activity, can be used for the prevention and treatment of diabetes. (by machine translation)

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