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N-(AMIDINOPHENYL) CYCLOUREA ANALOGS AS FACTOR XA INHIBITORS

The present application describes N-(amidinophenyl)cyclourea analogs of formula I: STR1 which are useful as inhibitors of factor Xa.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP

The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Palladium-catalysed reduction of heteroaromatic naphthyl ethers: Structural effects on reactivity

Tetrazolyl and benzisothiazolyl naphthylmethylic ethers 3 and 4(a-e) are stable crystalline compounds that can be synthesised in high yields by reaction of the corresponding naphthyl methanols (1a-e) with the derivatizing agents 2a and 2b. Experimental conditions for palladium-catalysed hydrogenolysis of ethers 3, 4, with a hydrogen donor and with molecular hydrogen, were investigated. Analysis of the structure and reactivity indicates that naphthylmethylic ethers 3 and 4 are structurally similar to the corresponding benzyloxyderivatives around the ether bond but exhibit different reactivity. Structural analysis for these compounds is based on crystallographic structure determinations, for 5-(2-naphthylmethoxy)-1-phenyltetrazole (3a) and 3-(2-naphthylmethoxy)-1,2- benzisothiazole 1,1-dioxide (4a), and molecular orbital DFT(B3LYP)/6-311G(d) calculations, for all ethers. It can be concluded from this investigation that 5-chloro-1-phenyltetrazole 2a acts as a better derivatizing agent for naphthyl methanols than 3-chloro-1,2-benzisothiazole-11-dioxide 2b, this contrasting with what has been observed with phenols, allylic and benzylic alcohols.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Effect of Steel Wires on the Microwave Pyrolysis of Tire Powders

The discharge caused by metals triggered by microwave radiation is a key issue, whereas little attention was paid to the pyrolysis of waste tires by using the interaction between microwave and metals. In this work, the effect of such factors, that is, the microwave power, the steel wire (SW) mass fraction, and its spatial position in the tire powders (TPs), as well as the flow rate of the carrier gas, on the pyrolysis of the samples were experimentally examined in a laboratory-scale microwave oven. It was observed that the addition of SWs significantly accelerated the pyrolytic reaction of the TPs with regard to the conversion rate (product yields), even at rather low power, which may lead to a more complete degradation and significant reduction in the economic cost of the process. In addition, the presence of SWs has significant effects on the composition of products with different phases, especially gas yield (up to 35.3%) and also the H2 concentration in tires (up to 16.11%) were extremely high. The research on the discharge triggered by metals subjected to microwave irradiation will be instructive for promoting the industrial applications of discharges due to microwave radiation.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Effect of fragmentation degree on sensory and texture attributes of cooked rice

This study investigated the possibility of classified utilization of broken rice by analyzing sensory and texture attributes of cooked rice with different fragmentations. Compared with head rice, the relative concentration of volatile components in broken rice with three fragmentations (25%, 50%, 75%) increased 21%, 43% and 26%, respectively. Among them, 50% fragmentation rice sample contained the greatest amount of typical rice related aroma compounds, including heptanal, hexanal, nonanal, 1-octen-3-ol, 1-pentanol and 2-pentylfuran. Moreover, 50% fragmentation could increase the taste intensity of fruitiness, nuttiness, toastiness and sweetness of cooked rice significantly. The hardness of cooked rice was found to be negatively related with fragmentation degree, while the stickiness and water soluble protein content were positively related with fragmentations. The results of this study suggest that suitable utilization of broken rice with 50% fragmentation has a potential to enhance desirable rice flavor and increase staple food supply. Practical applications: During rice processing, broken rice with different fragmentations will form inevitably, the composition of which is not different from head rice, but much cheaper. Broken rice with 50% fragmentation has a potential to add desirable rice flavor to cooked rice. Thus suitable utilization of broken rice could be applied to achieve high added-value of rice milling by-product.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Synthesis, characterisation and application of disperse dyes derived from N-2-hydroxyethyl-l-naphthylamine

The synthesis and characterisation of a series of disperse dyes obtained by diazotisation of heterocyclic arylamines and coupling of these compounds with N-2-hydroxyethyl-1-naphthylamine are reported. The dyes were applied to cellulose acetate and their dyeing and fastness properties were assessed and summarised. The absorption spectra of the dyes are discussed, with regard to structure and substitution of the heterocyclic diazo component.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

Brief introduction of Benzo[d]isothiazole

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Characterization of Aroma Compounds in Two Meat Flavorings Prepared from Thermal Reaction of Enzymatic Hydrolysates of Black Pig and Common White Pig Meat Proteinss with Oxidized Lard

Meat flavorings were prepared by thermal reactions of enzymatic hydrolysates of black pig and common white pig (large white) meat proteins with oxidized lard. The volatile compounds of the two meat flavorings were analyzed by solvent assistant flavor distillation (SAFE) combined with gas chromatography and mass spectrometry (GC-MS). Based on retention indices and mass spectra, a total of 123 volatile compounds, including sulfur-containing compounds, nitrogencontaining heterocycles, oxygen-containing heterocycles, aldehydes, ketones, alcohols, acids, esters and hydrocarbons, were identified. In comparison, the white pig meat-derived flavoring had a greater percentage (relative to the total peak area) of alkyl furanes, aliphatic aldehydes and acids while the black pig meat-derived flavoring had a greater percentage of sulfur-containing compounds, nitrogen-containing heterocycles, and esters. However, their relative contents of ketones and alcohols were similar. Furthermore, by gas chromatography-olfactometry (GC-O), a total of 31 odor-active compounds were identified through comparison of their retention indices and odor characteristics with those of authentic standards. Among them, 28 compounds were common to two meat flavorings, and in particular dimethyltrisulfide, furfuryl mercaptan, 3-ethyl-2,5-dimethylpyrazine, 3-(methylthio) propanal,2-ethylthiophene,(E,E)-2,4-decadienal,(E)-2-decenal,(E)-2-nonenal,1-octen-3-ol and 3-hydroxy-2-butanone had high flavor dilution (FD) factors. However, the number of compounds with high FD values was greater in the black pig meat-derived flavoring than in the white pig meat-derived flavoring. Additionally, the spider-web plots for the potent odor-active compounds revealed that the black pig meat-derived flavoring had higher scores for meaty and fatty odors than the black pig meat-derived flavoring, which could explain why the black pig meat-derived flavoring had stronger meaty aroma than the black pig meat-derived flavoring.

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

 

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Structural activity relationship and importance of benzothiazole derivatives in medicinal chemistry: A comprehensive review

Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activi-ties, with less toxic effects and their derivatives showed enhanced activities, which has proven Ben-zothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, anti-allergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes ben-zothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.

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

 

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Complete study of the pyrolysis and gasification of scrap tires in a pilot plant reactor

The pyrolysis and gasification of tires was investigated in a pilot plant reactor provided with a system for condensation of semivolatile matter. The study comprised experiments at 450, 750, and 1000C both in nitrogen and 10% oxygen atmospheres. In the gas phase, only methane and benzene yields increased with temperature until 1000C. In the liquids, the main components were styrene, limonene, and isoprene. The solid fraction (including soot) increased with temperature. Zinc content of the char decreased with increasing temperature. Analysis of the surface area of the solids showed that the area was similar in all cases to that of a commercial carbon black. The higher surface of the soot with respect to the chars was observed. The results coincided with published findings, i.e., kinetic severity function values would produce 0.2% of methane at 450C and 4.5% at 750-1000C.

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

 

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Recent progress in the discovery and development of DNA gyrase B inhibitors

New antibacterials that modulate less explored targets are needed to fight the emerging bacterial resistance. DNA gyrase and topoisomerase IV are attractive targets in this search. These are both type II topoisomerases that can cleave both DNA strands, and can thus alter DNA topology during replication or similar processes. Currently, there are no ATP-competitive inhibitors of these two enzymes on the market, as the only aminocoumarin representative, novobiocin, was withdrawn due to safety concerns. The search for novel ATP-competitive inhibitors is a focus of ongoing industrial and academical research. This review summarizes the recent efforts in the design, synthesis and evaluation of GyrB/ParE inhibitors. The various approaches to achieve improved antibacterial activities are described, with particular reference to Gram-negative bacteria.

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