Category: 2682-49-7

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Synthesis, molecular modelling, and preliminary anticonvulsant activity evaluation of novel naphthalen-2-yl acetate and 1, 6-dithia-4, 9-diazaspiro [4.4] nonane-3, 8-dione derivatives

The synthesis, pharmacological evaluation and molecular modelling study of novel naphthalen-2-yl acetate and 1, 6-dithia-4, 9-diazaspiro [4.4]nonane-3, 8-dione derivatives as potential anticonvulsant agents are described. The newly synthesized compounds were characterized by both analytical and spectral data. Alkylation of 1H-imidazole or substituted piperazine with 1-(2-naphthyl)-2-bromoethanone (2) gave naphthalen-2-yl 2-(1H-imidazol-1-yl) acetate (3) and naphthalen-2-yl 2-(substituted piperazin-1-yl) acetate (4?8). Moreover, condensation of naphthalen-2-yl 2-bromoacetate or 2-bromo-1-(naphthalen-2-yl) ethanone with hydrazine hydrate and acetylacetone resulted in the formation of the cyclic pyrazole products 9 and 13. Sonication of naphthalen-2-yl acetate (1) with 2-chloropyridine, 2-chloropyrimidine and 2-(chloromethyl) oxirane gave naphthalen-2-yl 2-(pyridin-2-yl) acetate (10), naphthalen-2-yl 2-(pyrimidin-2-yl) acetate (11) and naphthalen-2-yl-3-(oxiran-2-yl) propanoate (12) respectively. Cyclocondensation reaction of 2-iminothiazolidin-4-one (14) with thioglycolic acid, thiolactic acid and thiomalic acid gave 1, 6-dithia-4, 9-diazaspiro [4.4]nonane-3, 8-dione derivatives (15?17). The compounds were tested?in vivo?for the anticonvulsant activity by delaying strychnine-induced seizures. The diazaspirononane (17) and 1-(2-naphthyl)-2-bromoethanone (2) showed a high significant delay in the onset of convulsion and prolongation of survival time compared to phenobarbital. The molecular modelling study of anticonvulsant activity of synthesized compounds showed a CNS depressant activity via modulation of benzodiazepine allosteric site in GABA-A receptors.

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Electric Literature 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.

Synthesis and biological activities of some new spiro 1,2,4-triazole derivatives having sulfonamide moiety

A new series of spiro 1,2,4-triazoles 5-9a-j were prepared by the reaction of appropriate amidrazones 4 with cyclic ketones in catalytic amount of p-toluene sulfonic acid. The structures of the titled compounds have been elucidated by the elemental analysis and spectroscopic data (IR, 1H NMR, 13C NMR and MS). The biological activities of the prepared compounds were investigated using well-established methods from the literature.

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A perspective on thiazolidinone scaffold development as a new therapeutic strategy for toxoplasmosis

Toxoplasma gondii is one of the most successful parasites due to its ability to infect a wide variety of warm-blooded animals. It is estimated that one-third of the world?s population is latently infected. The generic therapy for toxoplasmosis has been a combination of antifolates such as pyrimethamine or trimethoprim with either sulfadiazine or antibiotics such as clindamycin with a combination with leucovorin to prevent hematologic toxicity. This therapy shows limitations such as drug intolerance, low bioavailability or drug resistance by the parasite. There is a need for the development of new molecules with the capacity to block any stage of the parasite?s life cycle in humans or in a different type of hosts. Heterocyclic compounds are promissory drugs due to its reported biological activity; for this reason, thiazolidinone and its derivatives are presented as a new alternative not only for its inhibitory activity against the parasite but also for its high selectivity-level with high therapeutic index. Thiazolidinones are an important scaffold known to be associated with anticancer, antibacterial, antifungal, antiviral, antioxidant, and antidiabetic activities. The molecule possesses an imidazole ring that has been described as an antiprotozoal agent with antiparasitic properties and less toxicity. Thiazolidinone derivatives have been reportedly as building blocks in organic chemistry and as scaffolds for drug discovery. Here we present a perspective of how structural modifications of the thiazolidinone core could generate new compounds with high anti-parasitic effect and less toxic results.

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Chemistry is traditionally divided into organic and inorganic chemistry. COA of 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

Mesoionic sydnone: A review in their chemical and biological properties

Various literature sources have documented sydnones as important molecules with exclusive chemical properties and a wide spectrum of bioactivities. Sydnone can be defined as a five-membered pseudo-aromatic heterocyclic molecule. Classically, 1,2,3-oxadiazole forms the main skeleton of sydnone. The molecule has delocalized balanced positive and negative charges. The five annular atoms share the positive charge and the enolate-like exocyclic oxygen atom bears the negative charge. The hydrogen atom at the position C4 was proved to have acidic and nucleophilic functionalities making the sydnone ring reactive towards electrophilic reagents. These unique chemical features enable sydnones to interact with biomolecules resulting in important therapeutic effects like anticancer, antidiabetic, antimicrobial, antioxidant and anti-inflammatory. Consequently, we aim from the current article to review the available chemical and pharmacological information on sydnone and its derivatives.

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Recent developments of quinolone-based derivatives and their activities against Escherichia coli

Escherichia coli (E. coli) is the most common pathogen in both hospital and community settings, and is capable of causing infections that can lead to serious consequences. Quinolones, one of the most common antibiotics in clinical use, are effective weapons to treat E. coli infections. However, the resistance of E. coli to quinolones develops rapidly and spreads widely. Thus, it has become increasingly urgent to enhance the potency of quinolones against both drug-susceptible and drug-resistant E. coli. This review aims to summarize the recent developments of quinolone derivatives with potential activity against E. coli, and to discuss the structure-activity relationship for further rationale design of this kind of derivatives.

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Synthesis of novel 2-Thioxothiazolidin-4-one and thiazolidine-2, 4-dione derivatives as potential anticancer agents

A variety of novel thiazolidine derivatives (2-Thioxothiazolidin-4-one and thiazolidine-2, 4-dione derivatives) have been prepared by using 2,4-diphenyl-2Hchromene- 3-carbaldehyde and its derivatives as starting materials. This is the first example of the preparation of thiazolidine derivatives through this novel method. Structure evolution of the resulting thiazolidine derivatives leads to anticancer agents. Our preliminary data for some model compounds on three cancer cell lines (MCF7, A549 and B-16) suggested reasonable anticancer activity against the A549 and B-16 cell lines, with IC50 values of 20.7 and 20.4 muM, respectively. This method is operationally simple and works with a diverse range of substrates.

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Modified Mg: Al hydrotalcite in the synthesis of oxazolidin-2-ones

The modified Mg: Al (3: 1) hydrotalcite has been found to be an efficient catalyst in the conversion of carbamates into oxazolidin-2-ones under mild reaction conditions. A wide variety of oxazolidin-2-ones were obtained with excellent chemical yield. The Royal Society of Chemistry 2005.

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Anti-inflammatory effects of novel thiazolidinone derivatives as bioactive heterocycles on raw264.7 Cells

The inhibition of the inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2) and nuclear factor-XB (NF-XB) production are research targets of attract in the field of anti-inflammatory drug development. Therefore, this study was designed to investigate the anti-inflammatory effects of novel thiazolidinone derivatives using a cellular model of lipopolysaccharide (LPS)-stimulated murine macrophage RAW 264.7. In the present study, five new derivatives (A to E) of thiazolidinone were synthesized and screened for anti-inflammatory activities. Cell viability of LPS-stimulated RAW 264.7 macrophages clearly decreased in <55 mug/mL of synthesized A-E compounds especially in the presence of C; therefore, up to 50 mug/mL of compounds were selected for the subsequent analysis. A majority of these compounds showed significant inhibition on the production of NO in LPS-stimulated macrophages in a dose-dependent manner. Compounds B and D (10-50 mug/mL) significantly inhibited LPS-induced NF-XB (p65) production in a dose-dependent manner. The effects of B and D on iNOS and COX-2 mRNA and protein expression in LPS-stimulated RAW 264.7 cells were detected by real time-PCR and western blot. B derivative significantly suppressed the iNOS and COX-2 mRNA level and as well as protein expression. Taken together, these results reveal that compound B as new thiazolidinone derivative decreased expression of the inflammatory-related signals (NO, iNOS and COX-2) through regulation of NF-XB; hence, this compound could be suggested as a novel therapeutic strategy for inflammation-Associated disorders. A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 2682-49-7 Reference£º
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Nitroimidazoles: Part V – 1-(1-Methyl-5-nitroimidazol-2-yl)-1,2,4-triazolidin-3,5-diones and Analogues

Condensation of 1-methyl-2-methylsulphonyl-5-nitroimidazole (1) with the sodium salts of triazolindiones affords the derivatives 2a-i; similiar reaction with the sodium salts of thiazolidinone, 2-iminothiazolidine, pyrrolidinone, oxazolidinone and its 2-methyl and 2-chloromethyl analogues leads to the formation of products 3-8 respectively.Under the reaction conditions 3 is opened by dimethylamide ion to form 10, and 6 by methyl sulfinate ion to provide 13 respectively.Additionally, 6 is hydrolysed to the amine (12).Cyclic sulphamides undergo reaction with 1 to provide nitroimidazoles (23-28).

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1H and 13C NMR study on some substituted azolidine derivatives

The 1H and 13C NMR spectra carried out on (where for R = H, X = NH, NMe, NEt, CH2, S, O; for R = Me, X = NMe, CH2; for R = Et, X = NEt) are reported.The comparison of these results with those obtained for the thionic and selonic isologues shows that sulphur and selenium have a greater deshielding effect on the ring than oxygen.The resonance of the carbons not involved in the ? system have been correlated with the ? charges calculated by the DEL RE method.

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