Category: 2682-49-7

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Syntheses, characterization and evaluation of some 3-(Benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-ones as antimicrobial agents

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

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STRUCTURAL CHARACTERIZATION OF SOME SUBSTITUTED AZOLIDINE MOLECULES: UPS PHOTOELECTRON SPECTROSCOPIC STUDIES

The He(I) photoelectron spectra of some heterocyclic penta-atomic rings containing carboamido, thiocarbamido or selenocarbamido groups are reported.Ab initio and CNDO/2 computational methods have been used to assign the first four ionized molecular orbitals, by comparison with previously studied related molecules.Structural effects in homologous series of compounds, particularly conjugation between N and C=Y (Y=O, S, Se) moiety, and the through-space interaction between ring heteroatoms are analyzed.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H226N | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of Thiazolidin-2-one, 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

5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, biological evaluation, and molecular docking studies

Background: Infectious diseases symbolize a global consequential strain on public health security and impact on the socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in crucial need for the discovery and development of novel entity for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using classical methods of organic synthesis. Results: All 20 synthesized compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species. It should be mentioned that all compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Furthermore, 18 compounds appeared to be more potent than streptomycin against Staphylococcus aureus, Enterobacter cloacae, Pseudomonas aeruginosa, Listeria monocytogenes, and Escherichia coli. Three the most active compounds 4h, 5b, and 5g appeared to be more potent against MRSA than ampicillin, while streptomycin did not show any bactericidal activity. All three compounds displayed better activity also against resistant strains P. aeruginosa and E. coli than ampicillin. Furthermore, all compounds were able to inhibit biofilm formation 2- to 4-times more than both reference drugs. Compounds were evaluated also for their antifungal activity against eight species. The evaluation revealed that all compounds exhibited antifungal activity better than the reference drugs bifonazole and ketoconazole. Molecular docking studies on antibacterial and antifungal targets were performed in order to elucidate the mechanism of antibacterial activity of synthesized compounds. Conclusion: All tested compounds showed good antibacterial and antifungal activity better than that of reference drugs and three the most active compounds could consider as lead compounds for the development of new more potent agents.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H312N | ChemSpider

Application of 2682-49-7, 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. 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS. In a Review£¬once mentioned of 2682-49-7

Progress and prospects on DENV protease inhibitors

New treatments are desperately required to combat increasing rate of dengue fever cases reported in tropical and sub-tropical parts of the world. Among the ten proteins (structural and non-structural) encoded by dengue viral genome, NS2B-NS3 protease is an ideal target for drug discovery. It is responsible for the processing of poly protein that is required for genome replication of the virus. Moreover, inhibitors designed against proteases were found successful in Human Immuno-deficiency Virus (HIV) and Hepatitis C Virus (HCV). Complete molecular mechanism and a survey of inhibitors reported against dengue protease will be helpful in designing effective and potent inhibitors. This review provides an insight on molecular mechanism of dengue virus protease and covers up-to-date information on different inhibitors reported against dengue proteases with medicinal chemistry perspective.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H467N | ChemSpider

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. COA of Formula: C3H5NOS. Introducing a new discovery about 2682-49-7, Name is Thiazolidin-2-one

Bis(benzofuran?thiazolidinone)s and bis(benzofuran?thiazinanone)s as inhibiting agents for chikungunya virus

There are currently still no approved antiviral drugs to treat or prevent chikungunya virus (CHIKV) infections despite the fact that this arbovirus continues to cause outbreaks in Africa, Asia, and South- and Central-America. Thus 20 new conjugated compounds in the families of bis(benzofuran?1,3-thiazolidin-4-one)s and bis(benzofuran?1,3-thiazinan-4-one)s were designed based on the structural features of suramin. These new compounds were synthesized by chemical methods and their structures were confirmed spectroscopically. In CPE reduction assays, six of these new bis-conjugates inhibited CHIKV replication in Vero E6 cells with EC50 in the range of 1.9?2.7 muM and selectivity index values of ?75 or higher. These results and compounds provide a starting point for further optimization, design, and synthesis of new antiviral agents for this (re)emerging disease.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H317N | ChemSpider

Chemistry is traditionally divided into organic and inorganic chemistry. Formula: C3H5NOS, 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

Hydrogen Bonding. Part 7. A Scale of Solute Hydrogen-bond Acidity based on log K Values for Complexation in Tetrachloromethane

A scale of solute hydrogen-bond acidity has been constructed using equilibrium constants (as log K values) for complexation of series of acids (i) against a given base in dilute solution in tetrachloromethane, equation (A). Forty-five such equations have been solved to yield LB and DB log Ki = LB log KAHi +DB (A) values characterising the base, and log KAH values that characterise the acid. In this analysis, use has been made of the novel observation that all the lines in equation (A) intersect at a given point where log K = log KAH = -1.1 with K on the molar scale. Some 190 log KAH values that constitute a reasonably general scale of solute hydrogen-bond acidity have been obtained. It is shown that there is no general connection between log KAH and any proton-transfer quantities, although certain family dependences are obtained. A number of acid-base combinations are excluded from equation (A), and alternative log KAHE values have been determined for such cases. The general log KAH values may be transformed into alpha2H values suitable for use in multiple linear-regression analysis through the equation alpha2H = (log KAH +1 .1 )/4.636.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H377N | ChemSpider

Synthetic Route of 2682-49-7, 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. 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS. In a Article£¬once mentioned of 2682-49-7

Synthesis, characterization and biological evaluation of thioureas, acylthioureas and 4-thiazolidinones as anticancer and antiviral agents

In this study, thiourea derivatives [1-4] were synthesized by using 2-amino-4-substituted pyridine compounds and these compounds have been used as the starting materials for synthesis of 2-imino-1,3-thiazolidin-4-one ring [5, 6]. Two different procedures for 4-thiazolidinone ring closure and synthesis method were optimized. The synthesized compounds were identified by the help of elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectral data while the purities of them were proved with TLC. Synthesized compounds were evaluated for their antiviral and anticancer activity. Antiviral activity against Murine norovirus, Yellow fever, Enterovirus and Chikungunya strains of the test compounds were investigated and EC50 values of these compounds were determined higher than 0,3 muM. Cytotoxicity of test compounds was examined on NIH3T3 cell line. When the anticancer activity of test compounds was examined against PC-3, A549, HeLa, HT-29, MCF-7, SJSA1 and K562 cell lines, the percent proliferation values of these compounds were observed over 61% for all cell lines.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H354N | ChemSpider

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. name: Thiazolidin-2-one, 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

Chemotherapy of breast cancer by heterocyclic compounds

Heterocyclic compounds are generally scattered in nature and occupy a prominent location in medicinal chemistry as pharmaceuticals and drug intermediates. They play a widespread role in the metabolism of living cells, and clinically used to treat diverse sicknesses. The healing significance of heterocyclics has created a much interest in the synthesis of latest heterocyclic machine instructions to look at the sulphur and nitrogen condensed biodynamic. Reviews of the pharmacological pastime of 1,2,4- triazole derivatives are presented. a few bi-heterocyclic compounds incorporating a 1,3,4-thiazole and 1,2,four-triazole ring are presented as antimicrobial dealers.1,2,4-triazole derivatives template is a privileged fragment in cutting-edge medicinal chemistry thinking about its wide pharmacological spectrum and liking for various bio-targets. It is among the usually occurring heterocyclic nuclei in many marine in addition to herbal plant merchandise possessing a wide variety of biological packages.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H384N | 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

Design, synthesis, and anticancer potential of the enzyme (PARP-1) inhibitor with computational studies of new triazole, thiazolidinone, – thieno [2, 3-d] pyrimidinones

Background: Thienopyrimidine, triazole and thiazolidinone derivatives have recently gained attention due to their effective pharmacological activities. They show antioxidant, antitumor, antimicrobial, antiviral, anti-inflammatory and analgesic properties. Objective: Synthesis of new ethyl 2-amino-4-isopropyl-5-methylthiophene-3-carboxylate (2) was used as a starting material to produce 2-mercapto-methylthienopyrimidinone (3), (4) and 2- hydrazinyl-methylthienopyrimidinone (5), through high yields and evaluating anticancer activities. Methods: A series of novel Schiff?s bases (6-9) were produced after treatment of (5) with aldehydes. Triazolopyrimidinones (6a, 7a, 8a, 9a) were produced from cyclization of benzylidene (6-9) using Br2 / AcOH or dry pyridine /Ac2O. Thiazolidinones (6b, 7b, 8b, 9b) were synthesized from benzylidene (6-9) with mercaptoacetic acid. Results: All the compounds were synthesized in good yields (55-85%) in a regularly actual system under mild condition. The new compounds have been established by means of diverse spectroscopic ways as IR, NMR and MS. The newly synthesized compounds were evaluated for their antiproliferative activity against the breast MCF-7 carcinoma cell line. Compound (7) showed promising anticancer activity with IC50 of 6.9 muM, and 40.8% of antioxidant effect as DPPH inhibition. Molecular docking of (7) showed deltaG values of-20.54 kcal/ mol and -25.60 kcal/ mol. Molecular dynamics simulation of (7) in complex with PARP-1 revealed RMSD of 3.00 a. Conclusion: The QSAR study confirmed the presence of a relationship between anticancer activity and subdivided surface area descriptors with coefficient r2 = 0.98 with high predictive power.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H209N | ChemSpider

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

Biochemical indicators of nephrotoxicity in blood serum of rats treated with novel 4-thiazolidinone derivatives or their complexes with polyethylene glycol-containing nanoscale polymeric carrier

The aim of this study was to compare the effect of new synthetic 4-thiazolidinone derivatives (potential anticancer compounds denoted as 3882, 3288 and 3833) and doxorubicin (positive control) in free form and in their complexes with synthetic polyethylene glycol-containing nanoscale polymeric carrier on the biochemical indicators of nephrotoxicity in blood serum of rats. The concentration of total protein, urea, creatinine, glucose, ions of sodium, potassium, calcium, iron and chloride was measured. It was found that after injection of the investigated compounds, the concentration of sodium cations and chloride anions in blood serum was increased compared with control (untreated animals). Doxorubicin?s injection was accompanied by a decrease in the concentration of iron cations. The concentration of total protein, urea and creatinine decreased under the influence of the studied compounds. Complexation of these antineoplastic substances with a synthetic polymeric nanocarrier lowered the concentration of the investigated metabolites substantially compared to the effect of these compounds in free form. The normalization of concentration of total protein, urea and creatinine in blood serum of rats treated with complexes of the studied compounds with the polymeric carrier comparing with increased concentration of these indicators at the introduction of such compounds in free form was found.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H345N | ChemSpider