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Heteroaryl-phenyl substituted factor Xa inhibitors

The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

Brief introduction of Benzo[d]isothiazole

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272-16-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS. In a Article, authors is Sindler-Kulyk, M.£¬once mentioned of 272-16-2

PHOTOCHEMISTRY OF BENZISOTHIAZOLES IN THE PRESENCE OF DIMETHYL ACETYLENEDICARBOXYLATE

1,2-Benzisothiazole gave upon irradiation in the presence of dimethyl acetylenedicarboxylate a mixture of cis- and trans-substituted phenylthioalkenes (II) and 7-cyano-2,3-dicarboxybenzothiophene.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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272-16-2, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS. In a Article, authors is Nabizadeh, Shahnaz£¬once mentioned of 272-16-2

Understanding the mechanism of [3 + 2] cycloaddition reaction of benzoisothiazole-2,2-dioxide-3-ylidene with nitrones

A theoretical investigation was carried out on the mechanism and regioselectivity of the [3 + 2] cycloaddition (32CA) reaction of benzoisothiazole-2,2-dioxide-3-ylidene with nitrone using Molecular Electron Density Theory through DFT calculations at B3LYP and wB97xD functionals with 6-31G(d,p) basis set in the gas phase and toluene. Hard and soft acids and bases principle, Parr functions, as well as potential energy surface analysis were utilized for studying the regio- and stereoselectivity of this reaction, and the obtained results are consistent with the experimental observations. The electron localization function analysis of the nitrone shows that there is a double bond between N and C in the absence of any carbenoid or pseudoradical center. Therefore, a zwitterionic structure for nitrone 2 can be suggested, expected that its 32CA reaction is zw-type. The noncovalent interactions topological analysis shows that the first sigma bond has been formed before reaching the TS, which is in line with a two-stage one-step mechanism.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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272-16-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS. In a Article, authors is Sanchez-Palomo£¬once mentioned of 272-16-2

Characterisation of free and glycosidically bound aroma compounds of la Mancha Verdejo white wines

The aroma of Verdejo La Mancha white wines was studied by instrumental and sensory analysis across five consecutive vintages to determine their typicity and quality. Free and glycosidically-bound aroma compounds were isolated by solid phase extraction (SPE) to later be analysed using gas chromatography-mass spectrometry (GC/MS). Seventy-four (74) free aroma compounds and thirty-six (36) bound aroma compounds were identified and quantified in La Mancha Verdejo wines oven this five year period. Based on the result, Verdejo white wines presents a complex chemical profile with a wealth of aromas in its aromatic composition. The sensory profile of Verdejo wines was evaluated by experienced wine-tasters and was characterised by fresh, citric, green apple, fruity and tropical fruit aroma descriptors. This study shows the first complete aromatic characterisation of La Mancha Verdejo white wines, also the data suggest that these wines present a great aromatic potential.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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THERMAL FISSION OF HYDROXYLAMINE DERIVATIVES WITH NEIGHBOURING-GROUP-PARTICIPATION BY THIOETHER FUNCTIONS: PREPARATION OF 1,2-BENZISOTHIAZOLES

Some of the factors influencing the preparation of 1,2-benzisothiazoles from 2-(alkylthio)phenyl-substituted oximes are discussed.Good yields of 3-aryl-1,2-benzisothiazoles 4 may be obtained from readily available precursors.Reaction takes place under particularly mild conditions when a t-butylthio function is situated anti to the leaving group at oxime-nitrogen and S-N overlap is not restricted by ring-strain in the transition-state.The corresponding N-methyl-hydroxamic acid derivatives 2 give good yields of 2-methyl-1,2-benzisothiazol-3(2H)-one 13 only when a t-butylthio substituent is present, e.g. in 2f.The ethylthio- and i-propylthio-analogues 2d and 2e give the vinylthioethers 12, while the methylthio derivatives 2a-c undergo a novel rearrangement to “Pummerer” esters.The preparation of the polycyclic compounds fluoreno<9,9a,1-cd>-1,2 thiazole 7 and 2,2′-bi(2H-fluoreno<9,9a,1-de>-1,3-thiazine) 8 is described.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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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 Review, the author is Garicano Vilar, Elena and a compound is mentioned, 272-16-2, Benzo[d]isothiazole, introducing its new discovery. 272-16-2

Volatile compounds of six species of edible seaweed: A review

Seaweeds are widely distributed throughout the world. Many seaweeds are of commercial importance with some consumed directly or used as an ingredient as they have functional, nutritional and/or organoleptic properties. Consumer acceptance of food is closely related to its sensory properties, of which flavor is of prime importance. A significant contributor to flavor is the aromatic volatile components present. This review focusses on the volatile components identified in commercially important edible macroalgae species consisting of four brown (Himanthalia elongata, Laminaria spp. including L. ochroleuca, and Undaria pinnatifida) and two red species (Porphyra umbilicalis and Palmaria palmata). In excess of 200 volatile compounds have been identified consisting of hydrocarbons, alcohols, aldehydes, ketones, acids, esters, furans, phenols and sulfur- containing compounds, among others present in minor quantities. The extraction/concentration conditions, chromatography and detection methodologies applied varied and impacted on the volatiles identified due to differences in their hydrophobicity, molecular weight and vapor pressure. This review highlights that considerable more information is required to identify volatile aromatic compounds in edible macroalgae and to identify those most likely to impact sensory perception. Such information could be used to aid new product development or widen applications of these seaweeds in the food or beverage sectors.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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272-16-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS. In a article£¬once mentioned of 272-16-2

Removal of pollutants and reduction of bio-toxicity in a full scale chemical coagulation and reverse osmosis leachate treatment system

Removals of pollutants and toxic organic compounds and reduction in bio-toxicity of leachate along an operating full-scale leachate treatment system utilizing chemical coagulation, sand filtration, microfiltration (MF) and reverse osmosis (RO) membrane were evaluated. High pollutant removals were achieved mainly by coagulation and sand filtration. Major toxic organic pollutants, i.e. DEHP, DBP and bisphenol A were removed by 100%, 99.6% and 98.0%. Acute toxicity test using water flea, Nile Tilapia and common carp and genotoxicity (Comet assay) were conducted to determine toxicity reduction in leachate along the treatment. Ammonia was found to be the main acute toxic compounds in leachate as determined by LC50 but the effect of organic substances was also observed. DNA damage in fish exposed to diluted raw leachate (10% of LC50) was found to be 8.9-24.3% and it was subsequently decreased along the treatment. Correlation between pollutants and its bio-toxicity was established using multivariable analyses.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.272-16-2. In my other articles, you can also check out more blogs about 272-16-2

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS, 272-16-2, In a Article, authors is Omojokun, Olasunkanmi S.£¬once mentioned of 272-16-2

Alkaloid extracts from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) inhibit phosphodiesterase-5, arginase activities and oxidative stress in rats penile tissue

The erectogenic potential of alkaloids extracted from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) was investigated in this study. Fresh leaves obtained from Bitter leaf and Black night shade were air-dried, pulverized, and extracted for alkaloids. The inhibitory potential of the alkaloid extracts on arginase and phosphodiesterase-5 (PDE-5) activities in rats penile tissue was determined in vitro. The antioxidant properties were also evaluated and the constituent alkaloids quantified using GC-MS. The alkaloid extracts inhibited arginase (0?30.51?mug/ml) and PDE-5 (0?133.69?mug/ml) activities in a concentration-dependent pattern. Similarly, the alkaloid extracts inhibited Fe2+-induced lipid peroxidation in rats penile tissues, scavenged DPPH, OH, and NO radicals as a function of concentration. GC-MS characterization revealed over 20 alkaloid compounds. The inhibition of PDE-5-, arginase-, pro-oxidant-induced lipid peroxidative-, and free radicals-scavenging activities by the alkaloids is suggestive of putative mechanisms underlying their therapeutic use for managing erectile dysfunction in folklore medicine. Practical applications: Alkaloids extracted from Black nightshade (Solanum nigrum) and Bitter leaf (Vernonia amygdalina) were characterized and investigated by standard procedures for inhibitory action against key erectile dysfunction-linked enzymes and antioxidant activity. The alkaloids inhibited erectile dysfunction-linked enzymes (arginase and PDE-5) and showed considerable antioxidant activity in a concentration-dependent manner. In view of this, we suggest the application of these results in the development of erectile dysfunction drugs in the pharmaceutical industry, with probable minimal or no adverse effect.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Processes for producing isothiazole derivatives

A method for producing a 1,2-benzisothiazole characterized by treating a 2-(alkylthio)benzaldehyde oxime with a halogen compound; a method for producing a 3-halo-1,2-benzisothiazole characterized by treating a 1,2-benzisothiazole with a halogenating agent; and a method for producing a 1-(1,2-benzisothiazol-3-yl)piperazine characterized by reacting the obtained 3-halo-1,2-benzisothiazoles with a piperazine. By the method of the present invention, 1,2-benzisothiazoles and 3-halo-1,2-benzisothiazoles, which are useful as intermediates for pharmaceutical compositions such as psychotropic agents, and 1-(1,2-benzisothiazole-3-yl)piperazines synthesized therefrom can be obtained in a high yield without using expensive starting materials by shorter and simpler process than conventional methods.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

The important role of Benzo[d]isothiazole

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SPECTROSCOPIC PROPERTIES AND PROTONATION EQUILIBRIA IN 1,2-BENZISOTHIAZOLES

The protonation equilibria of 1,2-benzisothiazoles, involving substituents at position 3, or the ring nitrogen at position 2, have been investigated by potentiometric and/or spectrophotometric methods.The values of the protonation constants (log Kobs) have been compared with values calculated according to the linear relationships of Barlin and Perrin.For compounds with substituents at position 3, the protonation constants have been determined potentiometrically.The presence of the benzisothiazole moiety induces an increase of base strength, with respect to that expected from the calculated substituent effects according to Barlin and Perrin.The protonation constants of the heterocyclic nitrogen at position 2 have been determined spectroscopically in very acidic solutions.The comparison of the values observed with those calculated following Barlin and Perrin for substituted isoquinoline shows that the ring nitrogen is less basic than expected.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com