Tag: M.W:300-400

Related Products of 7689-03-4, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 7689-03-4, Name is Campathecin, SMILES is [C@@]5(C2=C(C(N1CC4=C(C1=C2)N=C3C=CC=CC3=C4)=O)COC5=O)(CC)O, belongs to thiazines compound. In a article, author is Xu, Shu, introduce new discover of the category.

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.

Related Products of 7689-03-4, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 7689-03-4.

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

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 82911-69-1, Name is N-(9-Fluorenylmethoxycarbonyloxy)succinimide, molecular formula is C19H15NO5. In an article, author is Artym, Jolanta,once mentioned of 82911-69-1, Application In Synthesis of N-(9-Fluorenylmethoxycarbonyloxy)succinimide.

Topically applied azaphenothiazines inhibit contact sensitivity to oxazolone in mice

In this work we investigated the efficacy of two topically applied azaphenothiazine derivatives, 9-chloro-6-acetylaminobutylquinobenzo[3,2-b][1,4]thiazine (compound 4) and 6-chloroethylureido-ethyldiquino[3,2-b;2′;3′-e][1,4]thiazine (compound 5), in the amelioration of inflammatory symptoms of contact sensitivity (CS) to oxazolone in mice, in relation to the commercial ointment Protopic (R) (tacrolimus), the reference drug. The compounds were administered 24 h following elicitation of CS and, 24 h later, the parameters of inflammation, such as ear edema, blood composition, leukocyte level, numbers of cells in the draining lymph nodes, histological picture of the inflamed tissue, and the morphometric analysis, were analyzed. The study showed that the effectiveness of the studied azaphenothiazines applied as a 0.1% ointment was comparable to the reference drug regarding suppression of the inflammatory process, when all the investigated histological parameters are taken into account.

Interested yet? Keep reading other articles of 82911-69-1, you can contact me at any time and look forward to more communication. Application In Synthesis of N-(9-Fluorenylmethoxycarbonyloxy)succinimide.

Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – 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. 5460-09-3, Name is Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate, molecular formula is C10H8NNaO7S2. In an article, author is May, Lars,once mentioned of 5460-09-3, Recommanded Product: Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate.

Widely Electronically Tunable 2,6-Disubstituted Dithieno[1,4]thiazines-Electron-Rich Fluorophores Up to Intense NIR Emission

2,6-Difunctionalized dithieno[1,4]thiazines were efficiently synthesized by (pseudo)five- or (pseudo)three-component one-pot processes based on lithiation-electrophilic trapping sequences. As supported by structure-property relationships, the thiophene anellation mode predominantly controls the photophysical and electrochemical properties and the electronic structures (as obtained by DFT calculations). From molecular geometries and redox potentials to fluorescence quantum yields in solution, the interaction of the dithieno[1,4]thiazine-core with the substituents causes striking differences within the series of regioisomers. Most interestingly, strong acceptors introduced inanti-antidithieno[1,4]thiazines nearly induce a planarization of the ground-state geometry and a highly intense NIR fluorescence (phi(F)=0.52), whereas an equally substitutedsyn-syndithieno[1,4]thiazine exhibits a much stronger folded molecular structure and fluoresces poorly (phi(F)=0.01). In essence, electrochemical and photophysical properties of dithieno[1,4]thiazines can be tuned widely and outscore the compared phenothiazine with cathodically shifted oxidation potentials and redshifted and more intense absorption bands.

Interested yet? Keep reading other articles of 5460-09-3, you can contact me at any time and look forward to more communication. Recommanded Product: Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate.

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

 

Application of 82911-69-1, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 82911-69-1, Name is N-(9-Fluorenylmethoxycarbonyloxy)succinimide, SMILES is O=C(N1OC(OCC2C3=C(C4=C2C=CC=C4)C=CC=C3)=O)CCC1=O, belongs to thiazines compound. In a article, author is Bresnahan, Rebecca, introduce new discover of the category.

Sulthiame add-on therapy for epilepsy

Background This is an updated version of the Cochrane Review previously published in the Cochrane Database of Systematic Reviews 2015, Issue 10. Epilepsy is a common neurological condition, characterised by recurrent seizures. Most people respond to conventional antiepileptic drugs, however, around 30% will continue to experience seizures, despite treatment with multiple antiepileptic drugs. Sulthiame, also known as sultiame, is a widely used antiepileptic drug in Europe and Israel. We present a summary of the evidence for the use of sulthiame as add-on therapy in epilepsy. Objectives To assess the efficacy and tolerability of sulthiame as add-on therapy for people with epilepsy of any aetiology compared with placebo or another antiepileptic drug. Search methods For the latest update, we searched the Cochrane Register of Studies (CRS Web), which includes the Cochrane Epilepsy Group’s Specialized Register and CENTRAL (17 January 2019), MEDLINE Ovid (1946 to January 16, 2019), ClinicalTrials.gov and the WHO ICTRP Search Portal (17 January 2019). We imposed no language restrictions. We contacted the manufacturers of sulthiame, and researchers in the field to seek any ongoing or unpublished studies. Selection criteria Randomised controlled trials of add-on sulthiame, with any level of blinding (single, double or unblinded) in people of any age, with epilepsy of any aetiology. Data collection and analysis Two review authors independently selected trials for inclusion, and extracted relevant data. We assessed these outcomes: (1) 50% or greater reduction in seizure frequency between baseline and end of follow-up; (2) complete cessation of seizures during follow-up; (3) mean seizure frequency; (4) time-to-treatment withdrawal; (5) adverse effects; and (6) quality of life. We used intention-to-treat for primary analyses. We presented results as risk ratios (RR) with 95% confidence intervals (CIs). However, due to the paucity of trials, we mainly conducted a narrative analysis. Main results We included one placebo-controlled trial that recruited 37 infants with newly diagnosed West syndrome. This trial was funded by DESITIN Pharma, Germany. During the study, sulthiame was given as an add-on therapy to pyridoxine. No data were reported for the outcomes: 50% or greater reduction in seizure frequency between baseline and end of follow-up; mean seizure frequency; or quality of life. For complete cessation of seizures during a nine-day follow-up period for add-on sulthiame versus placebo, the RR was 11.14 (95% CI 0.67 to 184.47; very low-certainty evidence), however, this difference was not shown to be statistically significant (P = 0.09). The number of infants experiencing one or more adverse events was not significantly different between the two treatment groups (RR 0.85, 95% CI 0.44 to 1.64; very low-certainty evidence; P = 0.63). Somnolence was more prevalent amongst infants randomised to add-on sulthiame compared to placebo, but again, the difference was not statistically significant (RR 3.40, 95% CI 0.42 to 27.59; very low-certainty evidence; P = 0.25). We were unable to conduct meaningful analysis of time-to-treatment withdrawal and adverse effects due to incomplete data. Authors’ conclusions Sulthiame may lead to a cessation of seizures when used as an add-on therapy to pyridoxine in infants with West syndrome, however, we are very uncertain about the reliability of this finding. The included study was small and had a significant risk of bias, largely due to the lack of details regarding blinding and the incomplete reporting of outcomes. Both issues negatively impacted the certainty of the evidence. No conclusions can be drawn about the occurrence of adverse effects, change in quality of life, or mean reduction in seizure frequency. No evidence exists for the use of sulthiame as an add-on therapy in people with epilepsy outside West syndrome. Large, multi-centre randomised controlled trials are needed to inform clinical practice, if sulthiame is to be used as an add-on therapy for epilepsy.

Application of 82911-69-1, 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 82911-69-1.

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

 

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , HPLC of Formula: C19H15NO5, 82911-69-1, Name is N-(9-Fluorenylmethoxycarbonyloxy)succinimide, molecular formula is C19H15NO5, belongs to thiazines compound. In a document, author is Salah, Hanan, introduce the new discover.

Ring rearrangements and reactivity of 3-((4-oxo-4H-chromen-3-yl)methylene)-4-phenyl-1H-[1,5]benzodiazepin-2(3H)-one toward some nucleophiles

Condensation of 4-phenyl-1H-[1,5]benzodiazepin-2(3H)-one (1) with 3-formylchromone (2) afforded a mixture of 3-(chromenylmethylene)[1,5]benzodiazepinone 3 and 14-chromenyl-benzodiazepino[2,3: 6,5] pyrano[2,3-b] benzodiazepine 4. Ring rearrangements of compound 3 with different nucleophilic reagents, such as potassium hydroxide and/or ammonium acetate led to rearrangement into pyranobenzodiazepine 5 and pyridobenzodiazepine 6, respectively. Treatment of compound 3 with hydrazine hydrate, hydroxylamine hydrochloride, malononitrile, cyanothioacetamide, 2-cyano-3,3-disufanylacrylonitrile, and/or 2-cyano-3-phenylamino-3-sufanylacrylonitrile, has been carried out at different conditions, leading to versatile heterocyclic substituted benzodiazepines at position 3, viz. pyrazole 8, isoxazole 9, pyridines 10 and 11, 1,3-dithiine 12, and 1,3-thiazine 13 derivatives. (C) 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 82911-69-1. HPLC of Formula: C19H15NO5.

Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – 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. 5460-09-3, Name is Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate, molecular formula is C10H8NNaO7S2. In an article, author is Szakonyi, Zsolt,once mentioned of 5460-09-3, HPLC of Formula: C10H8NNaO7S2.

Stereoselective Synthesis and Antiproliferative Activity of Monoterpene-Fused 2-Imino-1,3-oxazines

Background: In the recent years the 2-imino-1,3-thiazine and 2-iminothiazolidine ring systems can be found as moieties in biologically relevant compounds, including BACE1 inhibitors, or cannabinoid receptor agonists, while monoterpene-based 2-imino-1,3-thiazines, prepared from chiral 1,3-amino alcohols exhibiting pronounced antiproliferative activity. Methods: The antiproliferative activities of the prepared compounds were determined in vitro against a panel of human adherent cancer cell lines including HeLa, MCF7 and A431 by MTT assay. Results: Starting from pinane-, apopinane-and carane-based beta-amino acid derivatives, 1,3-amino alcohols were prepared via two-step syntheses. The reactions of the product 1,3-amino alcohols and aryl isothiocyanates yielded gamma-hydroxythioureas, which were transformed to monoterpene-fused 2-imino-1,3-oxazines via base-catalysed ring closure. The antiproliferative activities of these 2-imino-1,3-oxazines were examined and the structure-activity relationships were studied from the aspects of the type and stereochemistry of the monoterpene ring and the substituent effects on the 1,3-oxazine ring system. The N-unsubstituted monoterpene-based derivatives exhibited considerable antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF7 and A431). Conclusions: A mild and efficient method has been developed for the synthesis of 2-imino-1,3-oxazines by the ring closure of thiourea adducts of 1,3-amino alcohols. The resulting 1,3-oxazines exert marked antiproliferative action on a panel of human cancer cell lines.

Interested yet? Keep reading other articles of 5460-09-3, you can contact me at any time and look forward to more communication. HPLC of Formula: C10H8NNaO7S2.

Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – 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. 5460-09-3, Name is Sodium 4-Amino-5-hydroxy-2,7-naphthalenedisulfonate, formurla is C10H8NNaO7S2. In a document, author is Jelen, Malgorzata, introducing its new discovery. Category: thiazines.

Lipophilicity estimation of anti-proliferative and anti-inflammatory 6-substituted 9-fluoroquino[3,2-b]benzo[1,4]thiazines

The lipophilicity parameters (logP(calcd), R-M0 and logP(TLC)) of 17 new anti-proliferative and anti-inflammatory tetracyclic 6-substituted 9-fluoroquinobenzothiazines were determined theoretically using computational methods and experimentally by reversed-phase thin-layer chromatography. The experimental parameter R-M0 was determined on the RP-18 silica plates with acetone-aqueous TRIS buffer as mobile phase. The obtained parameter R-M0 was further transformed into parameter logP(TLC) by use of the calibration curve. The theoretical logP(calcd) values differed depending on the substituents and nature of calculating programs. Fluoroquinobenzothiazines turned out to be rather middling or highly lipophilic compounds. The parameter R-M0 and specific hydrophobic surface area b were meaningly intercorrelated showing congeneric two classes of quinobenzothiazines. The calculated logP(calcd) and experimental logP(TLC) values were compared and intercorrelated to show different prediction power of the computational programs. The lipophilicity was correlated with molecular descriptors (molar mass, molar volume, and molar refractivity), biomolecular descriptors (HIA, PB, MDCK, Caco-2, and BBB) and in vitro tested biological activities (tumor necrosis factor alpha inhibition and antiproliferative activity). [GRAPHICS] .

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

 

Reference of 154127-42-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.154127-42-1, Name is (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide, molecular formula is C10H16N2O6S3. In a Patent£¬once mentioned of 154127-42-1

Process for the preparation of (R)-(+)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide.

Disclosed herein is an improved process for the preparation of (R)-(+)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide (Brinzolamide) and novel intermediates thereof.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 154127-42-1, help many people in the next few years.Reference of 154127-42-1

Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Related Products of 154127-42-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.154127-42-1, Name is (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide, molecular formula is C10H16N2O6S3. In a Patent£¬once mentioned of 154127-42-1

Sulfonamides useful as carbonic anhydrase inhibitors

Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 154127-42-1.

Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Synthetic Route of 154127-42-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.154127-42-1, Name is (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide, molecular formula is C10H16N2O6S3. In a Patent£¬once mentioned of 154127-42-1

IMPROVED PROCESS FOR THE PREPARATION OF (R)-(+)-4-(ETHYIAMINO)-3,4-DIHYDRO-2-(3- METHOXYPROPYL)-2H-THIENO[3,2-E]-L,2-THIAZINE-6-SULFONAMIDE-L,L-DIOXIDE

Disclosed herein is an improved process for the preparation of (R)-(+)-4- (Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6- sulfonamide- 1,1 -dioxide (Brinzolamide) and novel intermediates thereof.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 154127-42-1.

Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem