Sep 2021 News Top Picks: new discover of C20H16N2O4

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Dipyrimido[4,5-b:5,4-e][1,4]thiazine: synthesis and their enzyme inhibitory activity assessment on soybean 15-lipoxygenase

A series of new derivatives of dipyrimido[4,5-b:5,4-e][1,4] thiazine were synthesized by treatment of 5-amino-6-methyl-2-morpholino-4-pyrimidinethiol (1) with 5-bromo-2,4-dichloro-6-methylpyrimidine (2) in the presence of triethylamine and ethanol and subsequently with various secondary amines in EtOH/DMF. The thioether derivative 3 and heterocyclization products 4a-f were characterized by elemental analysis and spectroscopic techniques. The 15-LO inhibitory activities of the new synthesized compounds were also evaluated. The results show that compound 4e has the best IC50 of 15-LO inhibition (IC50 = 14.4 A mu M) but when all the products were theoretically docked into 15-LO, the GOLD scores of compounds 4e and 4d are 43.67 and 43.39 respectively, which show the best results. We suggest that the hydrogen bond interaction between Ser489 of 15-LO and the nitrogen of piperazine ring of compound 4e appears to play major role in lipoxygenase inhibition.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

1 Sep 2021 News Why Are Children Getting Addicted To C10H8NNaO7S2

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Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 5460-09-3, Name is Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate, belongs to thiazines compound, is a common compound. In a pantent, author is Siddiqui, Ruqaiyyah, once mentioned the new application about 5460-09-3, Recommanded Product: Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate.

Targeting SARS-CoV-2: Novel Source of Antiviral Compound(s) against COVID-19?

SARS-CoV-2 remains a significant burden on human health. Several lines of evidence suggest that surveillance of sewage and waste can provide an early warning sign for COVID-19 recurrence in a community. In support, SARS-CoV-2 traces were found in sewage in several countries. With this in mind, it is notable that pests, such as cockroaches, are exposed to pathogenic microbes routinely, yet thrive in polluted environments. Such species have likely developed mechanisms to protect themselves against pathogens. In support, recent studies showed that cockroaches possess potent antibacterial molecules to shield themselves from pathogenic bacteria. Among hundreds of molecules, some contained thiazine groups, imidazoles, chromene derivatives, isoquinoline group, sulfonamides, pyrrole-containing analogs, flavanones, and furanones. Here, we propose that cockroaches are a potential source of antiviral molecules to thwart infections. Because this is an unexploited resource for potential antivirals, we believe that cockroaches offer a unique source for novel bioactive molecule(s) to counter COVID-19 with huge clinical impact worldwide.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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New Advances in Chemical Research, May 2021. We’ll be discussing some of the latest developments in chemical about CAS: 82911-69-1, Name is N-(9-Fluorenylmethoxycarbonyloxy)succinimide, belongs to thiazines compound, is a common compound. In a pantent, author is Yin, Rong-Hua, once mentioned the new application about 82911-69-1, HPLC of Formula: https://www.ambeed.com/products/82911-69-1.html.

Two new compounds from Xanthium strumarium

One new lignan, fructusol A (1), and one new thiazine derivative, 2-hydroxy-xanthiazone (2), along with eight known ones, were isolated from the seeds of Xanthium strumarium. The structures of new compounds were elucidated on the basis of extensive spectroscopic methods. Meanwhile, compounds 1-3 were tested for their antifungal activities against Candida albicans (ATCC 10231) in vitro. No one showed obvious inhibitions (MIC90>128g/ml).

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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Oxicams Bind in a Novel Mode to the Cyclooxygenase Active Site via a Two-water-mediated H-bonding Network

Background: The oxicams are anti-inflammatory drugs targeting the cyclooxygenase enzymes. Results: Crystal complexes of mCOX-2isoxicam, mCOX-2meloxicam, and oCOX-1meloxicam are solved. Conclusion: Oxicams bind to the cyclooxygenase active sites in a novel mode. Significance: The first structural description of cyclooxygenase-oxicam complexes reveal a new binding pocket of inhibitors to cyclooxygenases. Oxicams are widely used nonsteroidal anti-inflammatory drugs (NSAIDs), but little is known about the molecular basis of the interaction with their target enzymes, the cyclooxygenases (COX). Isoxicam is a nonselective inhibitor of COX-1 and COX-2 whereas meloxicam displays some selectivity for COX-2. Here we report crystal complexes of COX-2 with isoxicam and meloxicam at 2.0 and 2.45 angstroms, respectively, and a crystal complex of COX-1 with meloxicam at 2.4 angstroms. These structures reveal that the oxicams bind to the active site of COX-2 using a binding pose not seen with other NSAIDs through two highly coordinated water molecules. The 4-hydroxyl group on the thiazine ring partners with Ser-530 via hydrogen bonding, and the heteroatom of the carboxamide ring of the oxicam scaffold interacts with Tyr-385 and Ser-530 through a highly coordinated water molecule. The nitrogen atom of the thiazine and the oxygen atom of the carboxamide bind to Arg-120 and Tyr-355 via another highly ordered water molecule. The rotation of Leu-531 in the structure opens a novel binding pocket, which is not utilized for the binding of other NSAIDs. In addition, a detailed study of meloxicamCOX-2 interactions revealed that mutation of Val-434 to Ile significantly reduces inhibition by meloxicam due to subtle changes around Phe-518, giving rise to the preferential inhibition of COX-2 over COX-1.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment., Category: thiazines, 82911-69-1, Name is N-(9-Fluorenylmethoxycarbonyloxy)succinimide, molecular formula is C19H15NO5, belongs to thiazines compound. In a document, author is Badrey, Mohamed G., introduce the new discover.

An Approach to Polysubstituted Triazipines, Thiadiazoles and Thiazoles Based on Benzopyran Moiety Through The Utility of Versatile Hydrazonoyl Halides as In Vitro Monoamine Oxidase Inhibitors

The chromene compound 1 is used as a key intermediate for synthesis of new heterocyclic compounds, and it reacted with hydrazonoyl chlorides in presence of TEA to give the amidrazone derivatives 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, which were cyclized to the corresponding triazepines 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h on boiling with sodium ethoxide. Conversion of compound 1 to the methylthiocarbamate derivative 6 was performed through its reaction with carbon disulfide and KOH followed by treatment with methyl iodide. Compound 6 reacted with hydrazonoyl chlorides in presence of TEA to give thiadiazoles 8a, 8b, 8c, 8d, 8e, 8f, 8g. In addition, chromene 1 combined with aminodithiocarbamic acid in DMF under reflux to furnish the thiosemicarbazide derivative 9, which in turn interacted with several hydrazonoyl chlorides to give the thiazole derivatives 11a, 11b, 11c, 11d, 11e. The structures of the prepared compounds were confirmed from their spectroscopic data and elemental analysis. The synthesized compounds were tested against both monoamine oxidase (MAO)-A and MAO-B and corrected to analyses showed good inhibitory activities especially against MAO-A.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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Thiazine Red(+) platelet inclusions in Cerebral Blood Vessels are first signs in an Alzheimer’s Disease mouse model

Strong evidence shows an association between cerebral vascular diseases and Alzheimer’s disease (AD). In order to study the interaction of beta-amyloid (A beta) plaques with brain vessels, we crossbred an AD mouse model (overexpressing amyloid precursor protein with the Swedish-Dutch-Iowa mutations, APP_SweDI) with mice expressing green fluorescent protein (GFP) under the flt-1/VEGFR1 promoter in vessels (GFP_FLT1). Our data show, that only very few A beta plaques were seen in 4-months old mice, focused in the mammillary body and in the lateral septal nucleus. The number of plaques markedly increased with age being most prominent in 12-months old mice. Thiazine Red was used to verify the plaques. Several Thiazine Red(+) inclusions were found in GFP(+) vessels, but only in non-perfused 4-months old mice. These inclusions were verified by Resorufin stainings possibly representing cerebral amyloid angiopathy. The inclusions were also seen in non-crossbred APP_SweDI but not in wildtype and GFP_FLT1 mice. In order to characterize these inclusions Flow Cytometry (FACS) analysis demonstrated that platelets were specifically stained by Thiazine Red(+), more pronounced when aggregated. In conclusion, our data show that Thiazine Red(+) inclusions representing aggregated platelets are a first pathological sign in AD before plaque development and may become important therapeutic targets in early AD.

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Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

Top Picks: new discover of C10H8NNaO7S2

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Synthesis and Antimicrobial Evaluation of some Functionalized Heterocycles Derived from Novel Quinolinyl Chalcone

The reaction of 3-acetyl-4-hydroxyl-1-methylquinolin-2(1H)-one (1) with 10-oxo-4,6,7,8,9,10-hexahydropyrazolo[1,5-a][1]benzothieno[2,3-d]pyrimidine-3-carbaldehyde (2) afforded the novel enone system 3. The latter compound was reacted with some 1,2-binucleophilic reagents to give pyrazoline derivative 4 and isoxazoline derivative 5. Treatment of chalcone 3 with 1,3-binucleophilic reagents afforded pyrimidine and thiazine derivatives 6-8. Moreover, reaction of compound 3 with active methylene reagents furnished pyridine, pyran, and cyclohexanone derivatives 9-12. Cyclization of compound 12 by using hydrazine hydrate yielded indazol-3-one derivative 13. On the other hand, the cyclocondensation of the enone 3 with 1,4-dinucleophilic reagents yielded diazepine derivative 14 and triazolothiadiazepine derivative 15. The characterization of the newly synthesized heterocyles were confirmed on the basis of their elemental analysis and spectral data (IR, NMR, and MS). These compounds were also screened for their antibacterial activities.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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Selective Construction of Diverse Polycyclic Spirooxindoles via a Three-Component Reaction of Cyclic Mercapto-Substituted beta-Enamino Esters, Isatins, and Cyclic 1,3-Diketones

The three-component reaction of alkyl 2-(benzo[b][1,4]thiazin-3-ylidene)acetates, isatins, and 1,3-indanedione (1,3-cyclopentanedione) in ethanol in the presence of acetic acid conveniently afforded spiro[indeno[1,2-b]phenothiazine-6,3′-indolines] or spiro[cyclopenta[b]phenothiazine-4,3′-indolines] in good yields and with high diastereoselectivity. More interestingly, a similar three-component reaction with 4-hydroxychromen-2-one resulted in the unexpected polycyclic spiro[benzo[b]chromeno[3′,4′:5,6]-pyrano[2,3-e][1,4]thiazine-7,3′-indolines] in satisfactory yields. A plausible reaction mechanism was rationally proposed for formation of different kinds of the spiro compounds, and the stereochemistries of the various spiro compounds were clearly elucidated.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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AIBN-Promoted Synthesis of Bibenzo[b][1,4]thiazines by the Condensation of 2,2′-Dithiodianiline with Methyl Aryl Ketones

A series of bibenzo[b][1,4]thiazines with various functional groups has been synthesized by a free-radical condensation reaction. Bibenzo[b][1,4]thiazines were obtained in moderate to good yield (up to 85%) through a one-step reaction of readily available 2,2′-dithiodianiline and methyl aryl ketones with AIBN as radical initiator in HOAc. Bibenzo[b][1,4]thiazines exhibit diversiform solid-state packing.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem

 

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Laccase mediator system obtained from a marine spore exhibits decolorization potential in harsh environmental conditions

Laccases play a significant role in remedying dye pollutants. Most of these enzymes are originated from terrestrial fungi and bacteria, thus they are not proper to be used in the environments with neutral/alkaline pH, or they may require laborious extraction/purification steps. These limitations can be solved using marine spore laccases through high stability and easy to use application. In the current study, laccase activity of the marine spore-forming Bacillus sp. KC2 was measured according to the guaiacol and syringaldazine oxidation. Abiotic stresses like pH of 6, temperature of 37 degrees C and 0.3 mM CuSO4 (in comparison with optimal sporulation conditions: pH of 8, temperature of 20 degrees C and 0.0 mM CuSO4) enhanced laccase formation in sporal coat. Maximum activity of enzyme was observed at 50 degrees C and pH 7, which did not change in the alkaline pH and temperature range of 20-70 degrees C. Results indicated ions, inhibitors and solvent stability of the enzyme and its activity were stimulated by Co2+, Mn2+, PMSF, acetone, acetonitrile, ethanol, and methanol. The spore laccase could decolorize synthetic dyes from various chemical groups including azo (acid orange, amaranth, trypan blue, congo red, and amido black), indigo (indigo carmine), thiazine (methylene blue, and toluidine blue), and triarylmethane (malachite green) with ABTS/syringaldazine mediators after 5 h. Degradation products were not toxic against Sorghum vulgare and Artemia sauna model organisms. The enzyme mediator system showed high potentials for dye bioremediation over a wide range of harsh conditions.

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Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem