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The high-field 1H NMR spectra of 1,3-propanesultams (2), 2,4-butanesultams (3) and 2,4-dimethyl-1,3-butadienesultams (6) are reported.Comparison of 2, 3 and 6 with 1,3-propanesultone (1) and 2,4-dimethyl-1,3-butadienesultone (5) reveals that the paramaggnetic shift induced by the NH group is smaller than that induced by oxygen.NMR spectra at lower temperatures show coupling effects with the NH proton.A half-chair conformation was deduced for 2,4-butanesultam from coupling constants and from a conformational analysis based on the R values, but a chair-chair interconversion could not be detected in the temperature range between 210 and 330 K.An unambiguous assignment was carried out for the methyl signals in the spectrum of 5 by homodecoupling experiments.

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Substituted thiourea condensed with chioroacetic acid in the presence of sodium acetate to form thiazolinonem and then reacts with aromatic aldehyde to give 5-benzylidene-4-thiazolidinone derivatives. Further thiazolidinone derivativesm react with methyliphenyl hydrazine to give Thiazolopyrazolines. The synthesized compounds were screened their antifungal activity against P. graminis and P. recondita at various concentrations, viz., 10, 100 and 1000 ppm.

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A series of innovative 5-(benzofuran-2-yl)-N?-(2-substituted-4-oxothiazolidin-3-yl)-1-phenyl-1H-pyrazole-3- carboxamide (4a-i) derivatives were synthesized by cyclocondensation reaction of various carbohydrazones (3a-i) with thioglycolic acid in DMF. The intermediate N?-(benzylidene)-5-(benzofuran-2-yl)-1- phenyl-1H-pyrazole-3-carbohydrazides (3a-i) was obtained by condensation of 5-(benzofuran-2-yl)-1-phenyl-1Hpyrazole- 3-carbohydrazide (1) with various substituted aromatic aldehydes (2a-i) in ethanol. The structures of newly synthesized compounds (4a-i) were corroborated through elemental analysis and spectral studies like IR, 1H NMR, 13C NMR and Mass spectra. The compounds were screened for their in-vitro antibacterial activity against a panel of pathogenic microorganism including gram-negative strains E. coli, P. vulgaris and S. typhi and grampositive bacterial strain, S. aureus at diverse concentrations and the result of bioassay was compared with Chloramphenicol.

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Background: Heterocyclic compounds have received much attention due to their versatile applications in the field of medicinal chemistry as well as organic chemistry. Objective: The main objective of this review is to give an overview of the recent application of beta-cyclodextrin catalyzed one?pot multicomponent reactions for the synthesis of different assemblies of heterocycles. Method: In this review, we have summarized the one-pot multicomponent approach towards the synthesis of heterocyclic compounds by using beta-cyclodextrin as a supramolecular catalyst. It is outlined under the headings (1) five-membered heterocyclic compounds and (2) six and seven membered heterocyclic compounds. Conclusion: This review outlined the recent key developments in the synthesis of different O-, N-and S-containing heterocyclic scaffolds, following MCRs published by using beta-CD and its derivatives as a supramolecular catalyst for the synthesis of five, six and seven membered heterocycles. The versatility of cyclodextrins and modified cyclodextrins will encourage chemists to develop new heterocyclic molecules by using multicomponent reactions in the near future.

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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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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. 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. Application of 2682-49-7

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Can You Really Do Chemisty Experiments About 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Regioselective Azidation of 2,4-Dichloroquinolines

Reactions of 2,4-dichloroquinolines (2a-f) with sodium azide in DMF lead either regioselectively to 4-azido-2-chloroquinolines (3a-f) or with excess of sodium azide and catalysts to 5-azido-tetrazolo<1,5-a>quinolines (4a-f). 2,4-Dichloroquinolines (2g-i) having electron donating substituents in 3-position react with sodium azide in DMF to a mixture of 4-azido-2-chloroquinolines (3g-i) and 5-chlorotetrazolo<1,5-a>quinolines (5g-i).When the reaction of the 2,4-dichloroquinolines (2a-i) with sodium azide is carried out in ethanol with addition of methanesulfonic acid, regioselectively 5-chloro-tetrazolo<1,5-a>quinolines (5a-i) are obtained.Structural assignments of 3 and 5 have been carried out by 13C-NMR spectra, IR spectra and degradation reactions of the azido- and tetrazolo group to aminoquinolines (7 and 10) via iminophosphoranes (8 and 9).It could be shown that in 2-azido/tetrazolo-quinolines (4 and 5) the tetrazole ring structure is the dominant species.

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Synthesis and biological evaluation of 4-thiazolidinone derivatives as antitubercular and antimicrobial agents

New series of N-[2-{2-(substitutedphenyl)-4-oxo-5-(substitutedbenzylidene)-1,3-thiazolidine}-iminoethyl]-2-amino-5-nitrothiazole, 5(a-m) have been synthesized from 2-amino-5-nitrothiazole as a starting material by conventional as well as microwave methods. All the synthesized compounds 4(a-m) were screened for their antibacterial and antifungal activities against some selected bacteria and fungi and antitubercular activity screened against Mycobacterium tuberculosis. The structure of all the synthesized compounds were confirmed by chemical and spectral analyses such as IR, 1H NMR, 13C NMR and FAB-Mass.

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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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Demethylation of 2,4-dimethoxyquinolines: the synthesis of atanine.

The synthesis of the quinoline alkaloid atanine 6, by selective demethylation of the 2,4-dimethoxyquinoline 11 is presented. An alternative demethylation utilising a thiolate anion leads to the regioisomeric 4-hydroxyquinoline 13.

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