Category: 2682-49-7

The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. An article , which mentions HPLC of Formula: C3H5NOS, molecular formula is C3H5NOS. The compound – Thiazolidin-2-one played an important role in people’s production and life., HPLC of Formula: C3H5NOS

The crystal structures of two closely related compounds, 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one, C15H18N2O3S, (1) and 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one 1,1-dioxide, C15H18N2O5S, (2), are presented. These compounds are comprised of three types of rings: thiazolidinone, nitrophenyl and cyclohexyl. In both structures, the rings are close to mutually perpendicular, with interplanar dihedral angles greater than 80 in each case. The thiazolidinone rings in both structures exhibit envelope puckering with the S atom as flap and the cyclohexyl rings are in their expected chair conformations. The two structures superpose fairly well, except for the orientation of the nitro groups with respect to their host phenyl ring, with a difference of about 10 between 1 and 2. The extended structure of 1 has two kinds of weak C – H?O interactions, giving rise to a closed ring formation involving three symmetry-related molecules. Structure 2 has four C – H?O interactions, two of which are exclusively between symmetry-related thiazolidinone dioxide moieties and have a parallel ‘give-and-take-fashion’ counterpart. In the other two interactions, the nitrophenyl ring and the cyclohexane ring each offer an H atom to the two O atoms on the sulfone group. Additionally, a C – H?pi interaction between a C – H group of the cyclohexane ring and the nitrophenyl ring of an adjacent molecule helps to consolidate the structure.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H489N | ChemSpider

New Advances in Chemical Research, May 2021. Application In Synthesis of Thiazolidin-2-one, Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Structural modification of the calcium antagonist fostedil (KB-944) and their coronary vasodilator activity are described.Amidophosphonate 4a-m, lactam amidophosphonate 7a-l, and diamide dilactam 10 were prepared, and their coronary vasodilator activity was assessed in dogs.Many compounds exhibited coronary vasodilator activity superior to that of fostedil.Among them, the 2-oxopyrrolidine derivative 7a was the most effective compound.Its action as a coronary vasodilator was 3 and 2 times more potent than that of fostedil and diltiazem hydrochloride, respectively.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H491N | ChemSpider

New Advances in Chemical Research, May 2021. Related Products of 2682-49-7, Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Background: The increasing predominance of microbial resistance towards available antimicrobial drugs urges the need to develop novel antimicrobial agents that will be effective against resistant bacteria and fungi. Objective: A series of 3-(benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-one derivatives were synthesized as pharmacophore hybrid of benzothiazole and thiazolidin-4-one moieties as exclusive antimicrobial agents. Methods: Proposed compounds were synthesized by four step reactions. First three steps involved synthesis of phenylthiourea, benzothiazol-2-ylamine and Schiff?s base srespectively. Finally, Schiff`s baseswere cyclized in the presence of thioglycolic acid to yield 4-thiazolidinone derivatives (2a-g), characterized by spectroscopic and elemental analysis. Resulted compounds were evaluated for their in vitro antimicrobial activities against four bacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and two fungal (A. niger and P. crysogenum) strains using agar diffusion method. The minimum inhibitory concentrations (MIC) of the synthesized compounds were also determined by tube dilution method. Results: All the compounds displayed good to moderate antimicrobial activity. Compound 2d was found most potent against Bacillus subtilis (MIC25mug/ml), whereas compound 2e was most active (MIC 25mug/ml) against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Conclusion: The compounds having electron-withdrawing groups in the phenyl ring exhibited promising activity. A correlation between the antimicrobial activity and Log P was also established. Most active compounds can be considered as the potential antibacterial agents and deserve further investigation for their pharmacological and toxicological profiling.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H296N | ChemSpider

New Advances in Chemical Research, May 2021. Safety of Thiazolidin-2-one, Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

A series of Thiazolidinone derivatives of 1,2-Benzisoxazole were synthesized. 4- hyroxy-2H-chromen-2-one is condensed with aromatic aldehyde to yield Schiff?s base which on cyclization with Mercapto acetic acid yields Thiazolidinone derivatives of Benzisoxazole. The structure of synthesized compounds has been established on the basis of their IR,1HNMR and Elemental analysis. The purity of the compounds was confirmed by TLC. The synthesized compounds were screened for In vitro antibacterial andantimicrobial activity by turbidimetric methods. Compounds 5b, 5d, 5e, 5i showed better antibacterial activity with the reference standard Ciprofloxacin and Compounds 5b, 5d, 5e, 5i showed good antimicrobial activity with the reference standard ketoconazole.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H416N | ChemSpider

The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. An article , which mentions Electric Literature of 2682-49-7, molecular formula is C3H5NOS. The compound – Thiazolidin-2-one played an important role in people’s production and life., Electric Literature of 2682-49-7

QSAR (Quantitative Structure-Activity Relationship) relate biological activity data along with the physiochemical and structural properties of a group of compounds. In general, most of the medicinal compounds involve heterocyclic compounds containing nitrogen and sulphur especially thiazolidinones they possess a broad spectrum antimicrobial activity. In the present study, we have carried out the QSAR studies of antimicrobial thiazolidinones using Hansch analysis. The results of QSAR studies indicated that the antimicrobial activity of thiazolidinones are mainly governed by the topological parameters, kiers 3rd order alpha shape index (kappa alpha 3) and second order valence connectivity index (2chinu) along with the lipophilic parameter, log of octanol water partition coefficient (log P).

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Quinuclidine – Wikipedia,
Quinuclidine | C7H449N | ChemSpider

Computed Properties of C3H5NOS, Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

Glucosinolates are found in plants of the order Brassicales and hydrolyzed to different breakdown products, particularly after tissue damage. In Barbarea vulgaris R.Br. (Brassicaceae), the dominant glucosinolate in the investigated ?G-type? is glucobarbarin, (S)-2-hydroxy-2-phenylethylglucosinolate. Formation of the nitrile from glucobarbarin was observed in vitro, while a previously suggested thioamide (synonym thionamide) was not confirmed. Resedine (5-phenyl-1,3-oxazolidin-2-one) was detected after glucobarbarin hydrolysis in crushed B. vulgaris leaves and siliques, but not in intact parts. The abundance increased for several hours after completion of hydrolysis. The corresponding 1,3-oxazolidine-2-thione (OAT), with the common name barbarin, was also formed, and appeared to be the precursor of resedine. Addition of each of two non-endogenous OATs, (S)-5-ethyl-5-methylOAT and (R)-5-vinylOAT (R-goitrin), to a leaf homogenate resulted in formation of the corresponding 1,3-oxazolidin-2-ones (OAOs), confirming the metabolic connection of OAT to OAO. Formation of OAOs was inhibited by prior brief heating of the homogenate, suggesting enzyme involvement. We suggest the conversion of OATs to OAOs to be catalyzed by an enzyme (?oxazolidinethionase?) responsible for turnover of OAT formed in intact plants. Resedine had been reported as an alkaloid from another species – Reseda luteola L. (Resedaceae) – naturally containing the glucosinolate glucobarbarin. However, resedine was not detected in intact R. luteola plants, but formed after tissue damage. The formation of resedine in two families suggests a broad distribution of putative OATases in the Brassicales; potentially involved in glucosinolate turnover that needs myrosinase activity as the committed step. In agreement with the proposed function of OATase, several candidate genes for myrosinases in glucosinolate turnover in intact plants were discovered in the B. vulgaris genome. We also suggest that biotechnological conversion of OATs to OAOs might improve the nutritional value of Brassicales protein. HPLC-MS/MS methods for detection of these glucobarbarin products are described.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H211N | ChemSpider

New Advances in Chemical Research in 2021. Reactions catalyzed within inorganic and organic materials interfaces commonly occur at high coverage, causing turnover rates to depend strongly on interfacial structure and composition, In a patent, 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery. Synthetic Route of 2682-49-7

Representatives of two classes of thiazolidine prodrug forms of the well-known radioprotective agents L-cysteine, cysteamine, and 2-[(aminopropyl)amino]ethanethiol (WR-1065) were synthesized by condensing the parent thiolamine with an appropriate carbonyl donor. Inherent toxicity of the prodrugs was assessed in V79 cells using a clonogenic survival assay. Protection against radiation-induced cell death was measured similarly after exposure to 0-8 Gy gamma (137Cs) radiation. Antimutagenic activity was determined at the hypoxanthine-guanine phosphoribosyltransferase (HGPRT) locus. All thiazolidine prodrugs exhibited less toxicity than their parent thiolamines, sometimes dramatically so. Protection against radiation-induced cell death was observed for the 2-alkylthiazolidine, 2(R,S)-D-ribo-(1?,2?,3?,4?-tetrahydroxybutyl) thiazolidine (RibCyst), which produced a protection factor at 8 Gy of 1.8; the cysteine analogue, 2(R,S)-D-ribo-(1?,2?,3?,4?-tetrahydroxybutyl) thiazolidine-4(R)-carboxylic acid (RibCys), was less active. RibCyst also exhibited excellent antimutational activity, rivaling that of WR-1065. The 2-oxothiazolidine analogues showed little activity in either determination under the conditions tested, perhaps due to their enhanced chemical and biochemical stability.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H482N | ChemSpider

Reference of 2682-49-7, Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

The present invention relates to novel compounds of the general formula (I) STR1 wherein R means hydrogen or C1-4 alkyl group; and Y stands for cyano, trifluoromethyl, aryloxy or aryl(C1-4 alkyl)oxy group. The compounds according to the invention show a gastric acid secretion-inhibiting effect and therefore, they are useful for the treatment of gastric and duodenal ulcers. In addition, they exert a cytoprotective action against gastric laesions induced, e.g. by indomethacin or acid-containing alcohol.

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Reference：
Quinuclidine – Wikipedia,
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Recommanded Product: 2682-49-7, Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

The present invention provides methods of screening an agent for activity using teleosts. Methods of screening an agent for angiogenesis activity, toxic activity and an effect cell death activity in teleosts are provided. Methods of screening an agent for an activity in the brain or central nervous system in zebrafish are provided. The invention further provides high throughput methods of screening agents in multi-well plates.

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Quinuclidine – Wikipedia,
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New Advances in Chemical Research in 2021. Reactions catalyzed within inorganic and organic materials interfaces commonly occur at high coverage, causing turnover rates to depend strongly on interfacial structure and composition, In a patent, 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery. Recommanded Product: 2682-49-7

BRD4 has recently emerged as a promising drug target. Therefore, identifying novel inhibitors with distinct properties could enrich their use in anticancer treatment. Guided by the cocrystal structure of hit compound 4 harboring a five-membered-ring linker motif, we quickly identified lead compound 7, which exhibited good antitumor effects in an MM.1S xenograft model by oral administration. Encouraged by its high potency and interesting scaffold, we performed further lead optimization to generate a novel potent series of bromodomain and extra-terminal (BET) inhibitors with a (1,2,4-triazol-5-yl)-3,4-dihydroquinoxalin-2(1H)-one structure. Among them, compound 19 was found to have the best balance of activity, stability, and antitumor efficacy. After confirming its low brain penetration, we conducted comprehensive preclinical studies, including a multiple-species pharmacokinetics profile, extensive cellular mechanism studies, hERG assay, and in vivo antitumor growth effect testing, and we found that compound 19 is a potential BET protein drug candidate for the treatment of cancer.

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Reference：
Quinuclidine – Wikipedia,
Quinuclidine | C7H314N | ChemSpider