Category: pyrrolines

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 5264-35-7, molcular formula is C5H9NO, introducing its new discovery. , 5264-35-7

N-ACYLPYRROLIDIN-2-YLALKYLBENZAMIDINE DERIVATIVES AS INHIBITORS OF FACTOR XA

This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

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1-Pyrroline | C4H7N – PubChem

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, 1081-17-0, name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, introducing its new discovery. 1081-17-0

Tissue-specific metabolite profiling of benzylisoquinoline alkaloids in the root of Macleaya cordata by combining laser microdissection with ultra-high-performance liquid chromatography/tandem mass spectrometry

Rationale: Tissue-specific metabolite profiling helps to find trace alkaloids masked during organ analysis, which contributes to understanding the alkaloid biosynthetic pathways in vivo and evaluating the quality of medical plants by morphology. As Macleaya cordata contains diverse types of benzylisoquinoline alkaloids (BIAs), the alkaloid metabolite profiling was carried out on various tissues of the root. Methods: Laser microdissection with fluorescence detection was used to recognize and dissect different tissues from the root of M. cordata. Ultra-high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry was applied to analyze the trace alkaloids in tissues. These detected alkaloids were elucidated using their accurate molecular weights, MS/MS data, MS fragmentation patterns and the known biosynthetic pathways of BIAs. Finally, the distribution of alkaloids in dissected tissues and whole sections was mapped. Results: Forty-nine alkaloids were identified from five microdissected tissues, and 24 of them were detected for the first time in M. cordata. Some types of alkaloids occurred specifically in dissected tissues. More alkaloids were detected in the cork and xylem vascular bundles which emit strong fluorescence under fluorescence microscopy. Some of the screened alkaloids were intermediates in sanguinarine and chelerythrine biosynthetic pathways, and others were speculated to be involved in the new branches of biosynthetic pathways. Conclusions: The integrated method is sensitive, specific and reliable for determining trace alkaloids, which is also a powerful tool for metabolite profiling of tissue-specific BIAs in situ. The present findings should contribute to a better understanding of the biosynthesis of BIAs in M. cordata root and provide scientific evidence for its quality evaluation based on morphological characteristics. Copyright

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.1081-17-0, you can also check out more blogs about1081-17-0

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Fuerstner, Alois and a compound is mentioned, 69778-83-2, 4-Methoxy-1H-pyrrol-2(5H)-one, introducing its new discovery. 69778-83-2

Total synthesis, molecular editing and evaluation of a tripyrrolic natural product: The case of “butylcycloheptylprodigiosin”

Conflicting reports are found in the literature on whether the ortho-pyrrolophane derivative 6, which has been named ” butylcycloheptylprodigiosin” even though it is a cyclononane derivative, is a natural product or merely a mis-assigned structure. This dispute has now been resolved by an unambiguous total synthesis of this complex alkaloid which confirms the initial structure assignment. The chosen approach is largely catalysis-based, featuring the first application of a “Narasaka-Heck” reaction in natural product chemistry. This palladium-catalyzed transformation allows the unsaturated oxime ester 26 to be converted into the bicyclic dihydropyrrole 27. Other notable reactions of the reported approach to 6 are a regioselective Tsuji-Trost reaction of the doubly allylic acetate 21 with methyl acetoacetate. a base-induced aromatization of 27 to the corresponding pyrrole 28. a chemoselective oxidation of the benzylic methyl group in 33 with cerium ammonium nitrate in a biphasic reaction medium that does not affect the labile pyrrole nucleus, and a Suzuki cross-coupling for the completion of the heterocyclic domain. Diversification in the latter step leads to a set of analogues that differ from the natural product in the terminal (hetero)arene ring. This structural modification results in complete loss of the very pronounced ability of the parent compound 6 to induce oxidative cleavage in double stranded DNA in the presence of Cu11. Several cyclononane-, cyclononene- and cyclononadiene derivatives prepared en route to 6 have been characterized by crystal structure analysis, allowing the conformational behavior of nine-membered carbocycles to be studied.

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Flosser, David A. and a compound is mentioned, 5264-35-7, 5-Methoxy-3,4-dihydro-2H-pyrrole, introducing its new discovery. 5264-35-7

Improved synthesis of dialkylaminopyrrolines

The literature synthesis of 5-dialkylamino-3,4-dihydro-2H-pyrroles from 5-methoxy-3,4-dihydro-2H-pyrrole has been much improved. In initial assays, the pyrrolinium salts obtained on alkylation of the dibutylaminoamidine are excellent “naked halide” catalysts.

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In an article, published in an article,authors is Beng, Timothy K., once mentioned the application of 73286-71-2, Name is N-Boc-2-pyrroline,molecular formula is C9H15NO2, is a conventional compound. this article was the specific content is as follows. 73286-71-2

Regiocontrolled synthesis of (hetero)aryl and alkenyl dehydropyrrolidines, dehydropiperidines and azepenes by Ru-catalyzed, heteroatom-directed alpha-C-H activation/cross-coupling of cyclic enamides with boronic acids

The synthesis of alpha-aryl and alkenyl pyrrolidine-, piperidine-, and azepane derivatives, through the intermediacy of cyclic enamides is described. The desired outcome is achieved through ruthenium-catalyzed, site-selective sp2 C-H activation/cross-coupling with aryl and alkenyl boronic acids. The regioselectivity (alpha-sp2vs. alpha-sp3vs. beta-sp2 C-H functionalization) is governed by the rate differences between sp2 and sp3 C-H activation and the necessity for chelation between the ruthenium metal and the carbonyl directing group.

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1081-17-0, In an article, published in an article,authors is Caballero-George, Catherina, once mentioned the application of 1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione,molecular formula is C11H9NO3, is a conventional compound. this article was the specific content is as follows.

Inhibitory activity on binding of specific ligands to the human angiotensin II AT1 and endothelin 1 ETA receptors: Bioactive benzo[c]phenanthridine alkaloids from the root of Bocconia frutescens

A bioassay-guided fractionation of the 80% ethanolic extract from Bocconia frutescens L. roots, showing a dose-dependent inhibitory effect towards both [3H]-angiotensin II and [3H]-BQ-123 binding to the human angiotensin II AT1 and endothelin 1 ETA receptors, led to an alkaloidal subfraction as the only responsible fraction for the activity of the whole extract. Among the alkaloids present in this fraction sanguinarine and chelerythrine were significant inhibitors of [3H]-angiotensin II binding (hAT1 receptor), with lC50 values within the micromolar range. On the contrary, the [3H]-BQ-123 binding (ETA receptor) was only weakly inhibited. Moreover, other members of the isoquinoline alkaloid family such as chelidonine and some protoberberine alkaloids exhibited no affinity for the two receptors, The present work shows the possible structure-activity relationship for these benzophenanthridine alkaloids on a screening bioassay using both stably transfected Chinese hamster ovary (CHO) and the human neuroblastoma SK-N-MC cells. Furthermore, the ability of these compounds to block AT1 and/or ETA receptors may provide some justification for the traditional use of Bocconia frutescens L. to control hypertension.

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69778-83-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 69778-83-2, Name is 4-Methoxy-1H-pyrrol-2(5H)-one, molecular formula is C5H7NO2. In a Article, authors is Patil, Sohan£¬once mentioned of 69778-83-2

Mitochondrial Impairment by Cyanine-Based Small Molecules Induces Apoptosis in Cancer Cells

Mitochondrion, the powerhouse of the cells, has emerged as one of the unorthodox targets in anticancer therapy due to its involvement in several cellular functions. However, the development of small molecules for selective mitochondrial damage in cancer cells remained limited and less explored. To address this, in our work, we have synthesized a natural product inspired cyanine-based 3-methoxy pyrrole small molecule library by a concise strategy. This strategy involves Vilsmeier and Pd(0) catalyzed Suzuki cross-coupling reactions as key steps. The screening of the library members in HeLa cervical cancer cells revealed two new molecules that localized into subcellular mitochondria and damaged them. These small molecules perturbed antiapoptotic (Bcl-2/Bcl-xl) and pro-apoptotic (Bax) proteins to produce reactive oxygen species (ROS). Molecular docking studies showed that both molecules bind more tightly with the BH3 domain of Bcl-2 proteins compared to obatoclax (a pan-Bcl-2 inhibitor). These novel small molecules arrested the cell cycle in the G0/G1 phase, cleaved caspase-3/9, and finally prompted late apoptosis. This small molecule-mediated mitochondrial damage induced remarkably high cervical cancer cell death. These unique small molecules can be further explored as chemical biology tools and next-generation organelle-targeted anticancer therapy.

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Pyrroline – Wikipedia,
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1122-10-7, Name is 3,4-Dibromo-1H-pyrrole-2,5-dione, belongs to pyrrolines compound, is a common compound. 1122-10-7In an article, authors is Barbosa, Filipa, once mentioned the new application about 1122-10-7.

Targeting antimicrobial drug resistance with marine natural products

The rise and spread of antimicrobial resistance represents one of the most pressing health issues of today. Antimicrobial resistance in micro-organisms can arise due to a multiplicity of factors, including permeability changes in the cell membrane, increase of drug efflux pumps, enzymatic modification or inactivation of the antibiotic, target site modification, alternative metabolic pathways and biofilm formation. The marine environment is a valuable source of diverse natural products with a huge variety of biological activities. Among them, antimicrobial compounds show promising biological activities against numerous drug-resistant bacteria and fungi, making marine natural products a very promising resource in the search for novel antimicrobial agents. This review summarises the state-of-art of marine natural products with antibacterial and antifungal properties against drug-resistant micro-organisms. These natural products were categorised based on their chemical structure, and their respective sources and activities are highlighted. The chemical diversity associated with these marine-derived molecules is enormous, including peptides, polyketides, alkaloids, sterols, terpenoids, lactones, halogenated compounds, nucleosides, etc., some of which have rare substructures. Some of the marine compounds mentioned do not have intrinsic antimicrobial activity but potentiate the antimicrobial effect of other antimicrobials via inhibition of efflux pumps. Although these agents are still in preclinical studies, evidence of their in vivo efficacy suggest research of new drugs from the ocean to overcome antimicrobial resistance in order to fulfil an unmet medical need.

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1081-17-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1081-17-0, Name is 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione, molecular formula is C11H9NO3. In a Article, authors is Slavik, Jiri£¬once mentioned of 1081-17-0

OCCURENCE OF MAGNOFLORINE AND CORYTUBERINE IN SOME WILD OR CULTIVATED PLANTS OF CZECHOSLOVAKIA

Magnoflorine was isolated for the first time from Adonis vernalis L., Clematis recta L. and Epimedium versicolor MORR., further also from Aquilegia sp., Caltha palustris L., Isopyrum thalictroides L., and Aristolochia clematitis L.It was detected in Adonis aestivalis L., Clematis vitalba L., Consolida regalis GRAY, and Helleborus viridis L.Corytuberine was isolated for the first time from Caltha palustris L. and detected in small amounts in Adonis vernalis, A.aestivalis, Aquilegia sp., Consolida regalis, Clematis recta, Eranthis hiemalis L., Helleborus foetidus L.,H. niger L., H.viridis, Isopyrum thalictroides, and Aristolochia clematitis.From Consolida regalis a quaternary alkaloid (iodide C22H34NO2I) was isolated as the main component, probably of diterpenoid type.A small amount of coptisine was isolated from Isopyrum thalictroides and Aquilegia sp.

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An article , which mentions 1081-17-0, molecular formula is C11H9NO3. The compound – 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione played an important role in people’s production and life., 1081-17-0

Liquid chromatography-tandem mass spectrometry simultaneous determination and pharmacokinetic study of fourteen alkaloid components in dog plasma after oral administration of Corydalis bungeana Turcz extract

A rapid and sensitive Ultra high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the simultaneous determination of fourteen alkaloids in beagle dog plasma after a single oral dose of the Corydalis bungeana Turcz (C. bungeana) extract selected bifendate as the internal standard (IS). The plasma samples were preprocessed by liquid-liquid extraction (LLE) with aether before separation on an Agilent SB-C18 column (1.8 mum, 150 ¡Á 2.1 mm) using a gradient elution program. The mobile phase consists of 0.2% acetic acid and acetonitrile at the flow rate of 0.3 mL/min. In the positive ion mode, the analytes were detected by multiple reaction monitoring (MRM). The results indicated that calibration curves for fourteen analytes have good linearity (R2 = 0.9904). The lower limits of quantification (LLOQ) of fourteen alkaloids and IS were all over 4.87 ng/mL and the matrix effects ranged from 94.08% to 102.76%. The mean extraction recoveries of Quality control samples at low (LQC), medium (MQC) and high (HQC) and IS were all more than 78.03%. The intra- and inter-day precision (R.S.D.%) also met the criterion, at the same time the deviation of assay accuracies (R.E) ranged from ?13.70% to 14.40%. The Tmax values of fourteen alkaloids were no more than 1 h. The range of Cmax was from 74.16 ¡À 8.71 to 2256 ¡À 255.9 ng/mL. The assay was validated in the light of the regulatory bioanalytical guidelines and proved acceptable, which was successfully applied to a pharmacokinetic study of these compounds in beagle dogs after oral administration of Corydalis bungeana Turcz extract.

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