Category: 2682-49-7

2682-49-7, Name is Thiazolidin-2-one, belongs to thiazolidine compound, is a common compound. Computed Properties of C3H5NOSIn an article, once mentioned the new application about 2682-49-7.

Targets and patented drugs for chemotherapy of chagas disease in the last 15 years-period

Background: The American trypanosomiasis, Chagas disease, is a parasitic infection typically spread by triatomine vectors affecting millions of people all over Latin America. Existing chemotherapy is centered on the nitroaromatic compounds benznidazole and nifurtimox that provide unsatisfactory results and substantial side effects. So, the finding and exploration of novel ways to challenge this neglected disease is a main priority. Methods: The biologic and biochemical progress in the scientific knowledge of Trypanosoma cruzi in the period comprising last 15-years has increased the identification of multiple targets for Chagas? disease chemotherapy. In the middle of the best encouraging targets for trypanocidal drugs, ergosterol biosynthesis pathway and cruzipain, a key cysteine protease (CP) of T. cruzi, have been pointed out. Unfortunately, recent clinical trials investigating the administration of pozoconazole and ravuconazole to chronic indeterminate Chagas disease patients revealed their inferiority compared to the standard drug Benznidazole. Results: In view of the information gained in the preceding years, a reasonable approach for the fast development of novel anti-T. cruzi chemotherapy would be focused on K777, the cysteine proteinase inhibitor (CPI) near to enter to clinical trials, and founded on the clinical evaluation of combination of known drugs with existing trypanocidal agents to obtain more efficiency and less secondary effects. Top series of xanthine have been recently identified as clinical candidate for Chagas disease. In addition, trypanothione biosynthesis, thiol-dependant redox and polyamine metabolism, the glycolytic, glyconeogenic, pentose phosphate, lipidic and polyisoprenoid biosynthetic pathways, and the enzymes from biosynthetic glycoconjugates pathways have been studied. Several specific enzymes from these particular biosynthetic pathways such as hypoxanthine-guaninephosphoribosyl-transferase and farnesyl-pyrophosphate synthase, among others, have also been broadly studied in T. cruzi. Novel synthesized anti-T. cruzi compounds with or without specific single or multi-target assigned are also described in detail. Conclusion: In summary, loans on anti-Chagas disease agents focused to specific parasite targets as their metabolic pathways or specific enzymes will be summarized. Targets will also be specifically discussed. Patent literature collected and published from 2000 to 2015, alleging inhibitors for specific T. cruzi targets or trypanocidal activity was achieved over the search database from Delphion Research intellectual property network including international patents and the European patent office, Espacenet.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H270N | ChemSpider

Related Products of 2682-49-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS. In a Article£¬once mentioned of 2682-49-7

Synthesis of new 1, 8-dioxo-octahydroxanthene derivatives containing 4-Thiazolidinone moiety

A series of novel 1, 8-dioxo-octahydroxanthene derivatives containing 4-thiazolidinone framework (4a-f) were synthesized through a four-step reaction starting from the reduction of nitro derivatives of 1, 8-dioxo-octahydroxanthenes. The resulting aminoxanthenes converted to thiourea derivatives via their reaction with methyl isothiocyanate. The final products were synthesized through the reaction of thiourea derivatives with dialkylacetylene dicarboxylates. All of the steps were carried out under easy and mild reaction conditions in the absence of expensive catalysts or esoteric starting materials. The structures of compounds 3a-c and the final products were characterized according to their physical constants, spectral data such as NMR, IR spectra and also elemental analysis.

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Quinuclidine | C7H426N | ChemSpider

Reference of 2682-49-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 2682-49-7, Name is Thiazolidin-2-one,introducing its new discovery.

Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity

As a part of our ongoing studies in developing new derivatives as antimicrobial agents we describe the synthesis of novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6(5H)ones.The twenty-five newly synthesized compounds were tested for their antimicrobial and antifungal activity. All compounds have shown antibacterial properties with compounds 1?9 showing the lowest activity, followed by compounds 10?14 while compounds 15?25 the highest antibacterial activity. Specific compounds appeared to be more active than ampicillin in most studied strains and in some cases more active than streptomycin. Antifungal activity in most cases also was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophore model for antifungal activity of two fungal species Aspergillus fumigatus and Candida albicans were performed.

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Quinuclidine | C7H468N | ChemSpider

Related Products of 2682-49-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

Thiazolidone derivative and application thereof (by machine translation)

Chloro-4 – [3 – 4-() cyclopropylamino) carbonylamino-] – 7 – carbonylmethoxy-6-(I) quinolinecarboxazolone and application thereof, and the structure accords with the formula of the compound of the general formula shown in the specification. The drug has weak drug effect under normal conditions, is unstable in a high free radical environment, and can generate molecules with stronger drug effect. The medicine has good drug effect and safety, and can be used for treating tumor drugs. (by machine translation)

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 2682-49-7 is helpful to your research. Related Products of 2682-49-7

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of Thiazolidin-2-one, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 2682-49-7

New derivatives of thiozolidinone, synthesis and characterization

The present work involved synthesis of new thiozolidinone derivatives,These derivatives could be divided into three type of compounds; quinolin-2-one[V]a,b ,Schiff bases[VI]a,b and imide compounds[VII]a-d. The reaction p-Hydroxyacetophenone with thiosemicarbazide led to formation thiosemicarbazon compound [II], the reacted of thiosemicarbazone with chloro acetic acid in CH3CO2Na led to yield 4- thiazelidinone compound[III] in addition, thiosemicarbazide was POCl3 to [III] give [IV] compound used intermediates to synthesis new compounds of reacted with two type of coumarin in glacial acetic acid to give quinolin-2-one[V]a,b, The later compound refluxing with different benzaldehyde in dry benzene and glacial acetic acid give Schiff bases[VI]a,b . While the reaction with four kind acid anhydride using dioxane awarded imid compounds [VII]a-d. The synthesized compounds were identified using FTIR and 1H NMR spectroscopy.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H326N | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C3H5NOS, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 2682-49-7, name is Thiazolidin-2-one. In an article£¬Which mentioned a new discovery about 2682-49-7

Glucosinolate turnover in Brassicales species to an oxazolidin-2-one, formed via the 2-thione and without formation of thioamide

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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Quinuclidine | C7H211N | ChemSpider

Reference of 2682-49-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 2682-49-7, Name is Thiazolidin-2-one,introducing its new discovery.

Exploring the interaction between epidermal growth factor receptor tyrosine kinase and some of the synthesized inhibitors using combination of in-silico and in-vitro cytotoxicity methods

Quinazoline derivatives are potent inhibitors of human epidermal growth factor receptor (EGFR) as anticancer agents. In this study, the cytotoxic effects of a new series of synthesized quinazoline derivatives were evaluated using MTT assay against MCF-7 and HT-29 cell lines. Using molecular docking, the binding modes of all compounds were analyzed at the binding site of EGFR. Based on the results, the compounds L1, L2, L4, L5, L6, L7, L10, L15, and L18 may be promising EGFR inhibitors based on docking score and hydrogen bonds. Consistent with the experimental data, Met769 is recognized as a key residue in the binding of potential inhibitors. According to the MTT cytotoxicity assays, Lipinski’s rule of five (RO5), absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters, and docking studies, three compounds L4, L15, and L10 with IC50 values of 80, 60, and 1 muM against the MCF-7 were selected for further comparative assessments. The dynamics of free EGFR, and selected ligand-EGFR complexes were investigated using molecular dynamics (MD) simulation studies. The results indicated that the three compounds bound to EGFR active site in a stable manner during the simulation through the formation of new hydrogen bonds with Phe699, Leu694, Gly700, Lys721, Met769, Arg817, and Asp831 with the superiority of compound L15. These features can promote future drug candidate designing to produce better derivatives in the search for the anticancer agents.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H397N | ChemSpider

Related Products of 2682-49-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

Multi-targeting anticancer agents: Rational approaches, synthetic routes and structure activity relationship

We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H453N | ChemSpider

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery. Formula: C3H5NOS

Synthesis and biological activity of some new thiazolidinone derivatives

The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] and [G10]. All the prepared compounds were characterized by FT-IR, 1H-NMR spectra, also biologically activity evaluated, the synthesized derivatives have been screened for their two species of bacteria were used in this study as tested organisms. These are Escherichia Coli (Gram negative) and staphylococcus (Gram positive).

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Quinuclidine | C7H216N | ChemSpider

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Formula: C3H5NOS, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS

Organic Phosphorus Compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as Potent Calcium Antagonistic Vasodilators

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.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Formula: C3H5NOS, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2682-49-7

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