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There are disclosed compounds of the formula, STR1 where n is 0, 1 or 2; A is STR2 where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, STR3 or aryl except that when R1 is STR4 or aryl, R2 is hydrogen, or alternatively R1 +R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3 +R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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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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The metabolites produced in leaves of the crucifers winter cress (Barbarea vulgaris) and upland cress (Barbarea verna) abiotically elicited were investigated and their chemical structures were elucidated by analyses of spectroscopic data and confirmed by syntheses. Nasturlexins C and D and their sulfoxides are cruciferous phytoalexins displaying antifungal activity against the crucifer pathogens Alternaria brassicicola, Leptosphaeria maculans and Sclerotinia sclerotiorum. The biosynthesis of these metabolites is proposed based on pathways of cruciferous indolyl phytoalexins. This work indicates that B. vulgaris and B. verna have great potential as sources of defense pathways transferable to agriculturally important crops within the Brassica species.

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5-Chloro-3-methyl-2-benzofuran carbohydrazide (4) upon treatment with potassium isothiocynate in presence of hydrochloric acid in water gave 5-chloro-3-methylbenzofuran-2-carbo-N-thiosemicarbazide (5). The cyclisation of 5-chloro-3-methylbenzofuran-2-carbo-N-thiosemicarbazide (5) under different reaction conditions offered 1,3,4-oxadiazole, 1,3,4-thiadiazole, 1,2,4-triazole, thiazolidinone and thiopyrimidinone. The structures of these compounds were established on the basis of spectral data. Some of these compounds exhibited good antimicrobial activity.

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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. Electric Literature of 2682-49-7

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Background: Thiazoldin-4-one derivatives have been a subject of significant scientific exploration due to their potent biological activity as anti-infective agents. Methods: In the present investigation, a number of imidazoles bearing thiazolidin-4-one derivatives have been synthesized by suitable reactions of imidazole involving formation of ester, hydrazide, hydrazone and thiazolidin-4-one derivatives. The synthesized compounds have been characterized by suitable spectroscopic methods. The compounds have been evaluated for their antibacterial, antifungal and anthelmintic activities. Results: Compounds 5o and 5p with a 4-nitro substitution were observed to be most active against Staphylococcus aureus and Pseudomonas fluorescens with zone of inhibition of 23.3±0.3 mm and 29.0±0.9 mm respectively. Compound 5n with a para dimethyl amino substitution was most active against B. subtilis and E. coli with zone of inhibtion 21.0±0.6 and 26.5±0.6 respectively. Compounds 5g and 5h with 3-hydroxy substitution were found to be the most active against C. albicans and C. glabrata. Compound 5j having a fluoro substitution exhibited most potent anthelmintic activity among the synthesized compounds. Conclusion: Most of the synthesized compounds have shown moderate to good activities. Results of the present investigation reveal that further scientific research can be undertaken on these compounds to reveal interesting structure activity relationships for optimum utilization of these compounds.

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Background: Thiazole is one of the leading heterocyclic five-member ring compounds that contain nitrogen and sulphur atom. Many natural and/or synthetic compounds contain thiazole as an essential moiety and possess diverse therapeutic activities. The thiazole ring was modified at different positions to generate new molecules with potent antibacterial activities. Thus, the present review enumerates the antibacterial importance of thiazole and its derivatives. Method: The mining of literature has been performed using different database which includes only peer-reviewed journals. The quality of retrieved papers was appraised using standard tools. Moreover, the significant papers were described in detail to focus on thiazole derivatives showing considerable antibacterial activity. Result: The present review describes the chemistry, SAR (Structure Activity Relationship) studies and antibacterial importance of thiazole with different synthetic procedures. Conclusion: This particular study certainly benefits the researchers interested in exploiting the antibacterial activity of thiazoles in search of novel agents.

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The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), STR1 wherein A stands for hydrogen, halogen or a C1-4 alkyl, C1-4 alkoxy or nitro group; and n is 0 or 1. The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.

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Among all heterocycles, the triazine scaffold occupies a prominent position, possessing a broad range of biological activities. Triazine is found in many potent biologically active molecules with promising biological potential like anti-inflammatory, anti-mycobacterial, anti-viral, anti-cancer etc. which makes it an attractive scaffold for the design and development of new drugs. The wide spectrum of biological activity of this moiety has attracted attention in the field of medicinal chemistry. Due to these biological activities, their structure-activity relationship has generated interest among medicinal chemists and this has culminated in the discovery of several lead molecules. The outstanding development of triazine derivatives in diverse diseases within very short span of time proves its magnitude for medicinal chemistry research. Therefore, these compounds have been synthesized as target structure by many researchers, and were further evaluated for their biological activities. In this review, we have compiled and discussed the biological potential of s-triazine derivatives, which could provide a low-height flying bird’s eye view of the triazine derived compounds to a medicinal chemist, for a comprehensive and target oriented information for the development of clinically viable drugs.

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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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