Tag: M.W:200-300

Electric Literature of 90-30-2, New discoveries in chemical research and development in 2021.The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 90-30-2, Name is N-Phenyl-1-naphthylamine, SMILES is N(C1=CC=CC=C1)C1=CC=CC2=C1C=CC=C2, molecular formula is C16H13N, belongs to thiomorpholine compound. In an article, author is Martynov, Alexander V., introduce new discover of the category.

An efficient method for preparation of earlier unknown S-oxide of 2(E),6(E)-bis(chloromethylidene)-4-thiomorpholinamine by oxidation of 2(E), 6(E)-bis(chloromethylidene)-4-thiomorpholinamine hydrochloride with hydrogen peroxide in H2O or EtOH/H2O followed by the reaction mixture neutralization with Na2CO3 has been described. Interaction of the S-oxide with acetaldehyde, butanal, benzaldehyde, 4-methoxybenzaldehyde and 4-pyridinecarboxaldehyde in EtOH, C6H6, in the mixture of acetonitrile and ethanol or ethanol and benzene affords the unknown hydrazones, N-organylmethylidene-2(E), 6(E)-bis(chloromethylidene)-4-thiomorpholinamine-1-oxides. [GRAPHICS] .

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Thiomorpholine – Wikipedia,
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New Advances in Chemical Research, May 2021. The prevalence of solvent effects has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and their interactions with reaction intermediates. In an article, author is Hamama, WS, once mentioned the application of 131-56-6, Name is (2,4-Dihydroxyphenyl)(phenyl)methanone, molecular formula is C13H10O3, molecular weight is 214.22, MDL number is MFCD00002277, category is thiomorpholine. Now introduce a scientific discovery about this category, Synthetic Route of 131-56-6.

2,3-Dihydro-1H-benzo[d]imidazole-2-thione (1) was subjected to a Mannich reaction with either dimethylamine, urotropine, morpholine, thiomorpholine, (+/-) 3,3,5 trimethylhexahydroazepine, piperazine or p-bromoaniline and formalin in different molar ratios to afford the Mannich bases. The reactivity of the Mannich base 5a towards indole was also investigated. In addition the condensation of hydroxymethyl derivative 10 with morpholine, benzimidazole, p-bromoaniline, tryptamine and aminiothiazole was achieved.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

COA of Formula: https://www.ambeed.com/products/123843-67-4.html, New discoveries in chemical research and development in 2021.The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 123843-67-4, Name is 4-Bromo-2,6-difluorobenzonitrile, SMILES is N#CC1=C(F)C=C(Br)C=C1F, molecular formula is C7H2BrF2N, belongs to thiomorpholine compound. In an article, author is Combourieu, B, introduce new discover of the category.

In order to see if the biodegradative pathways for morpholine and thiomorpholine during degradation by Mycobacterium aurum MO1 could be generalized to other heterocyclic compounds, the degradation of piperidine by this strain was investigated by performing H-1-nuclear magnetic rc:resonance directly with the incubation medium. Ionspray mass spectrometry, performed without purification of the samples, was also used to confirm the structure of some metabolites during morpholine and thiomorpholine degradation. The results obtained with these tyro techniques suggested a general pathway for degradation of nitrogen heterocyclic compounds by M. aurum MO1. The first step of the degradative pathway is cleavage of the C-N bond; this leads formation of an intermediary amino acid, which is followed by deamination and oxidation of this amino acid into a diacid. Except in the case of thiodiglycolate obtained from thiomorpholine degradation, the dicarboxylates are completely mineralized by the bacterial cells. A comparison with previously published data showed that this pathway could be a general pathway for degradation by other strains of members of the genus Mycobacterium.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Chemical Research Letters, May 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media. 131-56-6, Name is (2,4-Dihydroxyphenyl)(phenyl)methanone, molecular formurla is C13H10O3. In a document, author is Babu, K. Sudhakar, introducing its new discovery. Safety of (2,4-Dihydroxyphenyl)(phenyl)methanone.

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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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Chemical Research Letters, May 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media. 90-14-2, Name is 1-Iodonaphthalene, molecular formurla is C10H7I. In a document, author is Levin, Jeremy I., introducing its new discovery. Electric Literature of 90-14-2.

A variety of heterocyclic ring systems have been prepared as scaffolds for butynyloxyphenyl sulfonamide and sulfone hydroxamic acid inhibitors of TACE enzyme. All scaffolds provided highly active TACE inhibitors, but selectivity, and cellular activity was highly scaffold dependent.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process., SDS of cas: 131-56-6, 131-56-6, Name is (2,4-Dihydroxyphenyl)(phenyl)methanone, molecular formula is C13H10O3, belongs to thiomorpholine compound. In a document, author is Samzadeh-Kermani, A., introduce the new discover.

A novel catalytic reaction involving terminal alkynes, carbon disulfide, and aziridines has been described. In this transformation, silver-acetylides react with carbon disulfide and aziridines to form 1,4-thiomorpholine molecules in good yields. The optimum conditions developed using silver iodide and (i-Pr)(2)EtN in DMF at 70 degrees C. [GRAPHICS] .

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Thiomorpholine – Wikipedia,
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New research progress on 84-51-5 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 84-51-5, Name is 2-Ethylanthracene-9,10-dione, molecular formurla is C16H12O2. In a document, author is Biava, Mariangela, introducing its new discovery. Synthetic Route of 84-51-5.

A hit optimization procedure based on isosteric and bioisosteric replacement of decorating groups at both the N1 and the C5 phenyl rings of 1,5-diarylpyrroles led to identification of 4-((1-(4-fluorophenyl)-2-methyl- 5-(4-(methylthio) phenyl)-1H-pyrrol-3-yl) methyl) thiomorpholine that is characterized by a very high activity toward both Mycobacterium tuberculosis 103471 and H37Rv strains (MIC values of 0.125 mu g/mL), and a safe profile in terms of cytotoxicity (CC(50) of > 128 mu g/mL) and protection index (> 1000). Antitubercular activity and protection index of the new compound are comparable to those found for the current antitubercular drugs streptomycin and rifampin. (C) 2010 Elsevier Ltd. All rights reserved.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Reference of 3965-55-7, New discoveries in chemical research and development in 2021.Chemistry can be defined as the study of matter and the changes it undergoes. 3965-55-7, Name is Sodium 3,5-bis(methoxycarbonyl)benzenesulfonate, SMILES is O=S(C1=CC(C(OC)=O)=CC(C(OC)=O)=C1)([O-])=O.[Na+], belongs to thiomorpholine compound. In a article, author is Schindler, U, introduce new discover of the category.

The heme-enzyme soluble guanylyl cyclase (sGC) is an ubiquitous NO receptor, which mediates NO downstream signaling by the generation of cGMP. We studied the mechanism of action of the anthranilic acid derivatives 5-chloro-2-(5-chloro-thiophene-2-sulfonylamino-N-(4-(morpholine-4-sulfonyl)-phenyl)-benzamide sodium salt (HMR1766) (proposed international nonproprietary name, ataciguat sodium) and 2-(4-chloro-phenylsulfonylamino)4,5- dimethoxy-N-(4-(thiomorpholine-4-sulfonyl)-phenyl)-benzamide (S3448) as a new class of sGC agonists. Both compounds activated different sGC preparations (purified from bovine lung, or crude from human corpus cavernosum) in a concentration-dependent and quickly reversible fashion (EC50 = 0.5-10 mu M), with mixed-type activation kinetics. Activation of sGC by these compounds was additive to activation by NO donors, but instead of being inhibited, it was potentiated by the heme-iron oxidants 1H-[1,2,4]-oxdiazolo[3,4-a]quinoxalin-1-one (ODQ) and 4H-8-bromo-1,2,4-oxadiazolo(3,4-d) benz(b)(1,4) oxazin-1-one (NS2028), suggesting that the new compounds target the ferric heme sGC isoform. Protoporphyrin IX acted as a competitive activator, and zinc-protoporphyrin IX inhibited activation of heme-oxidized sGC by HMR1766 and S3448, whereas heme depletion of sGC by Tween 20 treatment reduced activation. Both compounds increased cGMP levels in cultured rat aortic smooth muscle cells; induced vasorelaxation of isolated endothelium-denuded rat aorta, porcine coronary arteries, and human corpus cavernosum (EC50 1 to 10 mu M); and elicited phosphorylation of the cGMP kinase substrate vasodilator-stimulated phosphoprotein at Ser239. HMR1766 intravenous bolus injection decreased arterial blood pressure in anesthetized pigs. All of these pharmacological responses to the new compounds were enhanced by ODQ and NS2028. Our findings suggest that HMR1766 and S3448 preferentially activate the NO-insensitive heme-oxidized form of sGC, which exists to a variable extent in vascular tissues, and is a pharmacological target for these new vasodilator drugs.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

New research progress on 93-11-8 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 93-11-8, Name is Naphthalene-2-sulfonyl chloride, molecular formurla is C10H7ClO2S. In a document, author is Battula, Kumara Swamy, introducing its new discovery. Safety of Naphthalene-2-sulfonyl chloride.

A series of new thirteen N-(3-Methoxyphenyl)thiomorpholine-2-carboxamide 1, 1-dioxide derived 1, 4-disubtituted 1, 2, 3-triazole hybrids (7a-7m) were synthesized by Cu (I) catalyzed cycloaddition reaction and well characterized by (HNMR)-H-1, (CNMR)-C-13, FTIR, mass spectral and elemental analysis data. All the hybrid compounds were subjected to invitro anticancer activity against three human cancer cell lines MCF-7, Hela and A-549 and 2-hydroxy phenyl, 2-methoxy phenyl and 3-methoxy phenyl substituted (7f, 7g and 7h) derivatives were found to possess potential antiproliferative activity.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

New research progress on 93-11-8 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 93-11-8, Name is Naphthalene-2-sulfonyl chloride, molecular formurla is C10H7ClO2S. In a document, author is Mezil, Lynda, introducing its new discovery. Reference of 93-11-8.

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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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem