Heterocyclic Building Blocks-Thiomorpholine

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Mezil, Lynda, once mentioned the application of 99-61-6, Name is 3-Nitrobenzaldehyde, molecular formula is C7H5NO3, molecular weight is 151.12, MDL number is MFCD00007249, category is thiomorpholine. Now introduce a scientific discovery about this category, Computed Properties of C7H5NO3.

Tumor Selective Cytotoxic Action of a Thiomorpholin Hydroxamate Inhibitor (TMI-1) in Breast Cancer

Background: Targeted therapies, associated with standard chemotherapies, have improved breast cancer care. However, primary and acquired resistances are frequently observed and the development of new concepts is needed. High-throughput approaches to identify new active and safe molecules with or without an a priori” are currently developed. Also, repositioning already-approved drugs in cancer therapy is of growing interest. The thiomorpholine hydroxamate compound TMI-1 has been previously designed to inhibit metalloproteinase activity for the treatment of rheumatoid arthritis. We present here the repositioning of TMI-1 drug in breast cancer. Methodology/Principal Findings: We tested the effect of TMI-1 on luminal, basal and ERBB2-overexpressing breast tumor cell lines and on MMTV-ERBB2/neu tumor evolution. We measured the effects on i) cell survival, ii) cell cycle, iii) extrinsic and intrinsic apoptotic pathways, iv) association with doxorubicin, docetaxel and lapatinib, v) cancer stem cells compartment. In contrast with conventional cytotoxic drugs, TMI-1 was highly selective for tumor cells and cancer stem cells at submicromolar range. All non-malignant cells tested were resistant even at high concentration. TMI-1 was active on triple negative (TN) and ERBB2-overexpressing breast tumor cell lines, and was also highly efficient on human and murine primary” ERBB2-overexpressing cells. Treatment of transgenic MMTV-ERBB2/neu mice with 100 mg/kg/day TMI-1 alone induced tumor apoptosis, inhibiting mammary gland tumor occurrence and development. No adverse effects were noticed during the treatment. This compound had a strong synergistic effect in association with docetaxel, doxorubicin and lapatinib. We showed that TMI-1 mediates its selective effects by caspase-dependent apoptosis. TMI-1 was efficient in 34/40 tumor cell lines of various origins (ED50: 0.6 mu M to 12.5 mu M). Conclusions/Significance: This is the first demonstration of the tumor selective cytotoxic action of a thiomorpholin hydroxamate compound. TMI-1 is a novel repositionable drug not only for the treatment of adverse prognosis breast cancers but also for other neoplasms.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Safety of Anthrone90-44-8, Name is Anthrone, SMILES is O=C1C2=C(C=CC=C2)CC3=CC=CC=C13, belongs to thiomorpholine compound. In a article, author is Rodriguez-Lozada, Josue, introduce new discover of the category.

QSAR and Molecular Docking Studies of the Inhibitory Activity of Novel Heterocyclic GABA Analogues over GABA-AT

We have previously reported the synthesis, in vitro and in silico activities of new GABA analogues as inhibitors of the GABA-AT enzyme from Pseudomonas fluorescens, where the nitrogen atom at the gamma-position is embedded in heterocyclic scaffolds. With the goal of finding more potent inhibitors, we now report the synthesis of a new set of GABA analogues with a broader variation of heterocyclic scaffolds at the gamma-position such as thiazolidines, methyl-substituted piperidines, morpholine and thiomorpholine and determined their inhibitory potential over the GABA-AT enzyme from Pseudomonas fluorescens. These structural modifications led to compound 9b which showed a 73% inhibition against this enzyme. In vivo studies with PTZ-induced seizures on male CD1 mice show that compound 9b has a neuroprotective effect at a 0.50 mmole/kg dose. A QSAR study was carried out to find the molecular descriptors associated with the structural changes in the GABA scaffold to explain their inhibitory activity against GABA-AT. Employing 3D molecular descriptors allowed us to propose the GABA analogues enantiomeric active form. To evaluate the interaction with Pseudomonas fluorescens and human GABA-AT by molecular docking, the constructions of homology models was carried out. From these calculations, 9b showed a strong interaction with both GABA-AT enzymes in agreement with experimental results and the QSAR model, which indicates that bulky ligands tend to be the better inhibitors especially those with a sulfur atom on their structure.

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. you can also check out more blogs about 90-44-8. Safety of Anthrone.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 13120-77-9, Name is 2-Methyl-5-nitroanisole, SMILES is C1=C(C=CC(=C1OC)C)[N+](=O)[O-], in an article , author is Deniz, Nahide Gulsah, once mentioned of 13120-77-9, Application In Synthesis of 2-Methyl-5-nitroanisole.

The Vinylic S-N Reactions of Nitrodienes with Heteroatom-Substituted Nuchleophilies and Their Structural Studies

Herein, we report the reactions of 1,1,2,4,4-pentachloro-3-nitro-1,3-butadiene 1a and (1Z)-1-bromo-1,2,4,4-tetrachloro-3-nitro-1,3-butadiene 1b with nitrogen- and sulfur-containing nucleophiles to obtain highly functionalized S-, S,S-, S,S,S-, S,O- and N,S-substituted-polyhalodiene-3-nitro-1,3-butadiene derivatives. Most of these reactions turned out to be highly selective with good to very good yields. All new compounds have been characterized by nuclear magnetic resonance spectroscopy, mass spectrometry, and Fourier transform infrared spectroscopy spectroscopic data. The molecular structures of the 3a and 21a due to its exceptional substitution pattern were evidenced by the X-ray single-crystal diffraction method.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

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. 81-64-1, Name is 1,4-Dihydroxyanthracene-9,10-dione, molecular formula is C14H8O4. In an article, author is Babu, K. Sudhakar,once mentioned of 81-64-1, HPLC of Formula: C14H8O4.

SYNTHESIS, CHARACTERISATION AND BIOLOGICAL EVALUATION OF SOME NOVEL QUINAZOLINE DERIVATIVES AS POTENTIAL ANTIMICROBIAL AGENTS

Objective: In search of new potential antimicrobial agents, the aim of the present study was to synthesize the series of Quinazoline analogs by a simple and accessible approach and evaluate for their antimicrobial activity. Methods: Synthetic methodology involves the reaction of an anthranilic acid (1) with urea toget -2,4 di hydroxyl quinazoline (2) intermediate, which were further treated with POCl3 to get 2,4 di chloro quinazoline (3) derivative. Next 2,4 di chloro quinazoline (3) reacts with hydrazine hydrate in methanol for 4 hrs to get compounds, which further reacts with different carboxylic acids in POCl3 a series of novel fused 1,2,4 triazole derivatives, which were reacts with 4-thiomorpholinoaniline (7) in acetic acid to give target compounds (8a-k) in good yields. Results: The structures of the synthesized compounds were provided by spectral analysis, and the Synthesised compounds were tested for their antimicrobial activity against different fungi and bacteria species in vitro. Conclusion: The results of the study reveal that the new compounds possess promising antimicrobial activities.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

84-51-5, Name is 2-Ethylanthracene-9,10-dione, molecular formula is C16H12O2, Name: 2-Ethylanthracene-9,10-dione, belongs to thiomorpholine compound, is a common compound. In a patnet, author is Theodosis-Nobelos, Panagiotis, once mentioned the new application about 84-51-5.

Anti-inflammatory and Hypolipidemic Effect of Novel Conjugates with Trolox and Other Antioxidant Acids

Objectives: A series of esters and amides, incorporating an antioxidant residue, such as trolox or caffeic acid, and various moieties with different biological activities, were synthesised. Results: The obtained compounds demonstrated considerable anti-inflammatory, radical scavenging and antioxidant action. Thus, they could reduce carrageenan-induced rat paw oedema by 31-60% at 150 mu mol/kg and inhibit rat microsomal membrane lipid peroxidation with IC50 values as low as 1.4 mu M which is much lower than that of trolox. Most of them could also inhibit soybean lipoxygenase. The thiomorpholine derivatives decreased significantly all lipidemic indices of Triton-induced hyper-lipidemia in rats. The most active, the caffeic acid derivative (6), decreases triglycerides, total cholesterol and low density lipoprotein, in the plasma of hyperlipidemic rats, by 70%, 67%, and 73%, respectively, at 150 mu mol/kg (i.p.). Conclusion: The synthesised compounds, designed to exhibit two or more pharmacological actions, may be considered useful in the study of agents addressed to conditions involving inflammation and oxidative stress.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 147-93-3, Name is 2-Mercaptobenzoic acid, formurla is C7H6O2S. In a document, author is CECCHETTI, V, introducing its new discovery. Safety of 2-Mercaptobenzoic acid.

6-AMINOQUINOLONES – A NEW CLASS OF QUINOLONE ANTIBACTERIALS

A series of quinolone- and 1,8-naphthyridone-3-carboxylic acids, designed by previous QSAR studies and characterized by an amino group at the C-6 position instead of the usual fluorine atom, were synthesized for the first time and evaluated for in vitro antibacterial activity. All of the synthesized compounds maintain good activity against Gram-negative bacteria (Pseudomonas aeruginosa excluded), and those compounds having a thiomorpholine group as the C-7 substituent also have good activity against Gram-positive bacteria. Some aspects of structure-activity relationships associated with the C-1, C-5, C-7, and C-8 substituents are also discussed. Derivatives 18g and 38g displayed the best activity with geometric mean MICs of 0.45 and 0.66-0.76 mu g/mL against Gram-negative and Gram-positive bacteria, respectively. This antimicrobial activity reflects their ability to inhibit bacterial DNA-gyrase. The results of this study show that, while the C-6 fluorine is still the preferred substituent, good activity can still be obtained by replacing it with an amino group.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 3068-76-6, Name is N-(3-(Trimethoxysilyl)propyl)aniline, SMILES is CO[Si](CCCNC1=CC=CC=C1)(OC)OC, in an article , author is Zhang, JY, once mentioned of 3068-76-6, Recommanded Product: 3068-76-6.

Lanthionine ketimine and S-(2-aminoethyl)-L-cysteine ketimine induce the tyrosyl phosphorylation of 45 kDa protein in parallel with its stimulation of superoxide generation in human neutrophils

Human peripheral blood polymorphonuclear leukocytes were preincubated with lanthionine, S-(2-aminoethyl)-L-cysteine, and some of their derivatives found in normal human urine and bovine brain, Among these compounds, lanthionine ketimine and to a lesser extent S-(2-aminoethyl)-L-cysteine ketimine enhanced the N-formyl-methionyl-leucyl-phenylalanine-induced superoxide generation. These ketimines induced tyrosyl phosphorylation of 45 kDa protein of cells. The tyrosyl phosphorylation was markedly increased with time, and the phosphorylation process was dependent on the concentration of both ketimines. However, lanthionine, 1,4-thiomorpholine-3,5-dicarboxylic acid, S-(2- aminoethyl)-L-cysteine and 1,4-thiomorpholine-3-carboxylic acid were without effect both on superoxide generation and on tyrosyl phosphorylation of 45 kDa protein, Lanthionine ketimine and S-(2-aminoethyl)-L-cysteine ketimine also enhanced superoxide generation induced by opsonized zymosan but not the one induced by arachidonic acid and phorbol 12-myristate 13-acetate. Ketimine-primed superoxide generation and tyrosyl phoshorylation of 45 kDa protein were inhibited by genistein, an inhibitor of protein tyrosine kinase, but not by 1-(5-isoquinoline sulfonyl)-2-methylpiperazine, an inhibitor of protein kinase C.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Related Products of 5437-45-6, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 5437-45-6, Name is Benzyl 2-bromoacetate, SMILES is O=C(OCC1=CC=CC=C1)CBr, belongs to thiomorpholine compound. In a article, author is Hiranrat, Asadhawut, introduce new discover of the category.

Tedaniophorbasins A and B-Novel Fluorescent Pteridine Alkaloids Incorporating a Thiomorpholine from the Sponge Tedaniophorbas ceratosis

Two new fluorescent pteridine alkaloids, tedaniophorbasins A (1) and B (2), together with the known alkaloid N-methyltryptamine, were isolated, through application of mass directed purification, from the sponge Tedaniophorbas ceratosis collected from northern New South Wales, Australia. The structures of tedaniophorbasins A and B were deduced from the analysis of 1D/2D NMR and MS data and through application of C-13 NMR DFT calculations. Tedaniophorbasin A possesses a novel 2-imino-1,3-dimethyl-2,3,7,8-tetrahydro-1H-[1,4]thiazino[3,2-g]pteridin-4(6H)-one skeleton, while tedaniophorbasin B is its 2-oxo derivative. The compounds show significant Stokes shifts (similar to 14,000 cm(-1)) between excitation and emission wavelengths in their fluorescence spectra. The new compounds were tested for bioactivity against chloroquine-sensitive and chloroquine-resistant strains of the malaria parasite Plasmodium falciparum, breast and pancreatic cancer cell lines, and the protozoan parasite Trypanosoma brucei brucei but were inactive against all targets at 40 mu M.

Related Products of 5437-45-6, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 5437-45-6 is helpful to your research.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Recommanded Product: 1-Naphthoic acid, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 86-55-5, Name is 1-Naphthoic acid, molecular formula is C11H8O2. In an article, author is Mahato, Mamata,once mentioned of 86-55-5.

Mononuclear homoleptic organotin(IV) dithiocarbamates: Syntheses, structures and antimicrobial activities

Six mononuclear organotin(IV) complexes of two dithiocarbamato ligands, [Ph3SnL1] (1), [Bu2Sn(L-1)(2)] (2), [Ph2Sn(L-1)Cl] (3), [Ph2Sn(L-1)(2)] (4), [Ph2Sn(L-2)(2)] (5) and [Ph3Sn(L-2)] (6) where L-1 = thiomorpholine-4-carbodithiolate and L-2 = 2,6-dimethylmorpholine-4-carbodithiolate have been synthesized in good yields. Both ligands and complexes 1-6 were characterized by elemental analyses, FT-IR spectroscopy, UV-visible spectroscopy and H-1, C-13{H-1} Sn-119{H-1} NMR spectroscopy. In addition, the solid-state structures of the complexes were established through single-crystal X-ray diffraction analyses. The Xray analyses reveal that the Sn(IV) center is five-coordinated in 1, 3 and 6. In complexes 2, 4 and 5, Sn(IV) is six-coordinated and occupies the center of a distorted octahedron. Moreover, an asymmetric coordination mode of the dithiocarbamato ligands was observed in all complexes. The optical properties and thermal stabilities of all complexes were investigated. All complexes were evaluated for their in vitro antimicrobial properties against E. coli. Complex 1 shows a maximal biological activity whereas the least activity is found for complex 6. (C) 2017 Elsevier B.V. All rights reserved.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Synthetic Route of 83-56-7, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 83-56-7, Name is Naphthalene-1,5-diol, SMILES is OC1=C2C=CC=C(O)C2=CC=C1, belongs to thiomorpholine compound. In a article, author is Mantelingu, Kempegowda, introduce new discover of the category.

Intramolecular [3+2]-Cycloadditions of Azomethine Ylides Derived from Secondary Amines via Redox-Neutral C-H Functionalization

Azomethine ylides are accessed under mild conditions via benzoic acid catalyzed condensations of 1,2,3,4-tetrahydroisoquinolines or tryptolines with aldehydes bearing a pendent dipolarophile. These intermediates undergo intramolecular [3 + 2]-cycloadditions in a highly diastereoselective fashion to form polycyclic amines with four new stereogenic centers. Challenging substrates such as piperidine, morpholine, and thiomorpholine undergo the corresponding reactions at elevated temperatures.

Synthetic Route of 83-56-7, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 83-56-7.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem