Top Picks: new discover of (S)-4-Isopropylthiazolidine-2-thione

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Reference of 76186-04-4, 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, 76186-04-4, molcular formula is C6H11NS2, introducing its new discovery.

Desulfurilative self-coupling reaction of 1,3-thiazolidine-2-thiones and intramolecular non-bonded S?S interaction in the crystallographic structure of the products

An attempt at an asymmetric Pummerer-type reaction of trans-4-benzyloxythiane-1-oxide (1) with 3-trifluoroacetyl-4S-isopropyl-1,3-thiazolidine-2-thione (2) resulted in failure but an attractive desulfurilative self-coupling reaction of 4S-isopropyl-1,3-thiazolidine-2-thione (6) occurred to give 4S-isopropyl-3-(4S-isopropyl-1,3-thiazolin-2-yl)-1,3-thiazolidine-2-thione (5). The same desulfurilative self-coupling reaction of compound 6 or 11 efficiently proceeded by treatment of diphenyl sulfoxide (7a) or methyl phenyl sulfoxide (7b) with 2 or 3-trifluoroacetyl-1,3-thiazolidine-2-thione (8) to afford each corresponding product 5 or 9. Eventually, we found a practically useful method for the synthesis of 5 and 9 by exploiting TiCl4 and sodium salt 12 or 13 of 1,3-thiazolidine-2-thiones. Interestingly, intramolecular non-bonded S?S interactions were recognized in the crystallographic structures of 5 and 9.

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Electrochemical Oxidative C(sp3)?H/N?H Cross-Coupling for N-Mannich Bases with Hydrogen Evolution

N-Mannich bases are an important structure in various functional molecules. A new protocol to synthesize N-Mannich bases was established through electrochemical external-oxidant-free C(sp3)?H/N?H cross-coupling with hydrogen evolution. Various N-methylanilines were explored in this transformation. Moreover, simple amides, heteroatom-containing amides, and succinimides were well tolerated in moderate-to-good yields. In addition, the electrochemical dehydrogenative C(sp3)?H/N?H cross-coupling could be scaled up to 5 mmol. By using triethyl phosphite as trapping agent, the phosphorylation product was detected. At the same time, kinetic isotope effect experiments showed that the cleavage of the C?H bond is the rate-limiting step.

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Nitroimidazoles: Part XVI – Some 1-Methyl-4-nitro-5-substituted Imidazoles

Treatment of 1-methyl-4-nitro-5-chloroimidazole (3) with 5-membered lactames, e.g. imidazolidinones, oxazolidinone and thiazolidinone affords N-imidazolyl derivatives (4a-d).Reaction of 3 with imidazole yields 4e; amino derivatives (4f-h) are similarly obtained. 2-Hydroxypyrazine, 4-hydroxyquinazoline and 3,4,5-trichlorophenol and 3 react to form O-derivatives (4i-k).Imidazole (11) is formed from 1-methyl-4-chloro-5-nitroimidazole (10).

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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.

Organic selenium compounds as potential chemotherapeutic agents for improved cancer treatment

Selenium(Se)-containing compounds have attracted a growing interest as anticancer agents over recent decades, with mounting reports demonstrating their high efficacy and selectivity against cancer cells. Typically, Se compounds exert their cytotoxic effects by acting as pro-oxidants that alter cellular redox homeostasis. However, the precise intracellular targets, signalling pathways affected and mechanisms of cell death engaged following treatment vary with the chemical properties of the selenocompound and its metabolites, as well as the cancer model that is used. Naturally occurring organic Se compounds, besides encompassing a significant antitumor activity with an apparent ability to prevent metastasis, also seem to have fewer side effects and less systemic effects as reported for many inorganic Se compounds. On this basis, many novel organoselenium compounds have also been synthesized and examined as potential chemotherapeutic agents. This review aims to summarize the most well studied natural and synthetic organoselenium compounds and provide the most recent developments in our understanding of the molecular mechanisms that underlie their potential anticancer effects.

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Application 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.

An update on chemical classes targeting ERK1/2 for the management of cancer

Cancer, still in the limelight due to its dreadful nature, shows overexpression of multiple signaling macromolecules leading to failure of many chemotherapeutic agents and acquired resistance to chemotherapy. These factors highlight the significance of shifting toward targeted therapy in cancer research. Recently, ERKs (ERK1 and 2) have been established as a promising target for the management of various types of solid tumors, due to their aberrant involvement in cell growth and progression. Several ERKs inhibitors have reached clinical trials for the management of cancer and their derivatives are being continuously reported with noteworthy anticancer effect. This review highlights the recent reports on various chemical classes involved in the development of ERKs inhibitors along with their in vitro and in vivo activity and structure-activity relationship profile.

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Synthesis, characterization, biological evaluation and molecular docking studies of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides

Background: A series of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger by tube dilution method. The in vitro cytotoxicity study of the compounds was carried out against human colorectal (HCT116) cell line. The most promising anticancer derivatives (5l, 5k, 5i and 5p) were further docked to study their binding efficacy to the active site of the cyclin-dependent kinase-8. Results: All the compounds possessed significant antimicrobial activity with MIC in the range of 0.007 and 0.061 muM/ml. The cytotoxicity study revealed that almost all the derivatives were potent in inhibiting the growth of HCT116 cell line in comparison to the standard drug 5-fluorouracil. Compounds 5l and 5k (IC50 = 0.00005 and 0.00012 muM/ml, respectively) were highly cytotoxic towards HCT116 cell line in comparison to 5-fluorouracil (IC50 = 0.00615 muM/ml) taken as standard drug. Conclusion: The molecular docking studies of potent anticancer compounds 5l, 5k, 5i and 5p showed their putative binding mode and significant interactions with cyclin-dependent kinase-8 as prospective agents for treating colon cancer.

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Electric Literature of 5908-62-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5908-62-3, Name is 1,1-Dioxo-isothiazolidine, molecular formula is C3H7NO2S. In a Patent£¬once mentioned of 5908-62-3

NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE

Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.

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Synthesis, characterization and antimicrobial screening of some novel 5-(benzofuran-2-yl)-N?-(2-substituted-4-oxothiazolidin-3-YL)-1-phenyl-1hpyrazole- 3-carboxamide derivatives

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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So3h-functionalized zeolite-y as an efficient nanocatalyst for the synthesis of n-benzimidazole-2-aryl-4-thiazolidinones and tri-substituted imidazoles

Background: SO3H-functionalized zeolite-Y was prepared and used as a catalyst for the synthesis of 2-aryl-N-benzimidazole-4-thiazolidinones and tri-substituted imidazoles at ambient conditions. Objective: The goals of this catalytic method include excellent yields and high purity, inexpensive procedure and ease of product isolation, the use of nontoxic and heterogeneous acid catalyst, shorter reaction times and milder conditions. Materials and Methods: NMR spectra were recorded on Brucker spectrophotometer using Me4Si as internal standard. Mass spectra were recorded on an Agilent Technology 5975C VL MSD with tripe-axis detector. FT-IR spectra were obtained with KBr disc on a galaxy series FT-IR 5000 spectrometer. The surface morphology of nanostructures was analyzed by FE-SEM (EVO LS 10, Zeiss, Carl Zeiss, Germany). BET analysis were measured at 196 C by a Japan Belsorb II system after the samples were vacuum dried at 150C overnight. Results: The NSZ was characterized by FT-IR, FESEM, EDX, XRF, and BET. The catalytic activity of NSZ was investigated for synthesis of 1,3-tiazolidin-4-ones in H2O/Acetone at room temperature. Moreover, NSZ was used for synthesis of tri-substituted imidazoles at 60 C via solvent-free condensation. Different kinds of aromatic aldehydes were converted to the corresponding of products with good to excellent yields. Conclusion: Sulfonated zeolite-Y was as an efficient catalyst for the preparation of N-benzimidazole-2-aryl-1,3-thiazolidin-4-ones and 2,4,5-triaryl-1H-imidazoles. High reaction rates, elimination toxic solvent, simple experimental procedure and reusability of the catalyst are the important features of this protocol.

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Electric Literature of 185137-29-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.185137-29-5, Name is (S)-4-Phenylthiazolidine-2-thione, molecular formula is C9H9NS2. In a Article£¬once mentioned of 185137-29-5

Synthesis and Fungicidal Activity of Simple Structural 1,3-Thiazolidine-2-Thione Derivatives

A series of simple structural 1,3-thiazolidine-2-thione derivatives with various substituents on the S-, N-, 4-, and 5-positions was synthesized with high yields from various vicinal amino alcohols via two steps and screened for their antifungal activity. Bioassay results reveal that some thiazolidine-2-thione derivatives show strong antifungal activities against P. capsici, G. zeae, S. sclerotiorum, A. alternata, B. cinerea, or R. solani. The SAR analysis indicates that N-acyl substituted and 4-alkyl substituents can enhance the antifungal activity. Notably, 4-isopropyl-N-propionylthiazoldine-2-thione shows excellent activity against B. cinerea and G. zeae with IC50 values at 3.7 g/mL and 6.5 g/mL, respectively, and 4-isobutyl-N-propionylthiazoldine-2-thione shows remarkable fungicidal activity against R. solani, S. sclerotiorum, and G. zeae with IC50 values at 1.0 g/mL, 12.1 g/mL, and 11.0 g/mL, respectively. GRAPHICAL ABSTRACT.

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