Awesome and Easy Science Experiments about 1,1-Dioxo-isothiazolidine

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NOVEL TETRAHYDROPYRAZOLOPYRIDINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES

The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R5 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.

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Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents

A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling.

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Some scientific research about 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Synthesis of new 2-, 3-, and 4-substituted azidoquinolines: Inhibitors of human blood platelet aggregation in vitro

A series of 2-, 3- and 4-substituted azidoquinoline derivatives were synthesized and tested for their ability to inhibit human platelet aggregation in vitro triggered by adenosine diphosphate (15 muM), collagen (5 mug/ml), platelet activating factor (10 muM), or the stable prostaglandin H2 mimetic, U46619 (4 muM). The most active compounds (IC50 2.5-68.3 muM) were the geminal 3,3-diazides (4f and 4g) and the 4-azido-3-nitroquinolines (6f and 6g).

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Synthesis of new azobenzene dyes clubbed with thiazolidinone moiety and their applications

Purpose: The purpose of this paper is to synthesize some new azobenzene dyestuffs clubbed with thiazolidinone moiety and their solicitation in dyeing polyester fabrics representing their antibacterial evaluation. Design/methodology/approach: Herein, the authors report the synthesis of new thiazolidinone moiety after the coupling of diazotized 4-aminoacetophenone with resorcinol. The newly synthesized dyes were characterized by IR, elemental analysis, mass spectroscopy and proton nuclear magnetic resonance (1H NMR) spectral studies. The characteristics of dyeing of these dyestuffs were evaluated at optimum conditions. Concurrent with dyeing of polyester fabric for synthesized dyes with their antibacterial activity was estimated. Antimicrobial activity of the dyed fabrics at different concentrations was evaluated against gram-positive and gram-negative bacteria. Findings: Synthesized azobenzene dyestuffs clubbed with thiazolidinone dyes were applied on polyester fabrics. It was remarked that the modified dyes exhibited better colourfastness properties. Furthermore, the synthesized dyes revealed antimicrobial activity against gram-positive and gram-negative bacteria. Research limitations/implications: The synthesized azobenzene dyes for polyester dyeing were not bore earlier. Practical implications: The azobenzene dyes were accountable for giving improved colourfastness properties on polyester fabrics. Social implications: The synthesized azobenzene derivatives are sensibly expensive and applicable dyes accompanied with good antimicrobial and anticancer activities. Originality/value: A common process could be affording textiles of colour and antibacterial assets. The newly synthesized dyes containing thiazolidinone moieties with azobenzene coupler showed interesting disperse colourant for polyester with good antibacterial activity.

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Methods of screening agents for activity using teleosts

The present invention provides methods of screening an agent for activity using teleosts. Methods of screening an agent for angiogenesis activity, toxic activity and an effect cell death activity in teleosts are provided.

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Evaluation of hypoglycemic effects of 4-thiazolidinones

Nicotinic acid, a well-known hypolipidemic drug, is known to produce elevation of blood glucose in humans. In an earlier study in our laboratory, a thiazolidinone derivative of nicotinic acid was shown to exert hypolipidemic effect. The present study was aimed to find out if this compound produced any elevation of blood glucose in normal and diabetic Wistar rats. A closely related thiazolidinone was also evaluated. The two compounds reduced blood glucose in both normal and diabetic rats, while nicotinic acid produced hyperglycemia. The thiazolidinone structure with its hypoglycemic potential may be opposing the glucose elevating effect of nicotinoyl moiety. It is concluded from the study that the thiazolidinone derivative of nicotinic acid is a hypoglycemic agent besides being hypolipidemic. Detailed investigation is warranted.

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Archives for Chemistry Experiments of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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ARYL-SUBSTITUTED IMIDAZOLES AND METHODS OF MAKING AND USING SAME

The compounds of the invention are antagonists of MDM2 and/or MDMX, with excellent specificity for MDM2 and/or MDMX over other proteins. Several analogs demonstrate selective binding affinity to MDMX over MDM2. The disclosed compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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The Absolute Best Science Experiment for 76186-04-4

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Diastereoselective and Catalytic alpha-Alkylation of Chiral N-Acyl Thiazolidinethiones with Stable Carbocationic Salts

Direct nickel-catalyzed alkylation of chiral N-acyl-4-isopropyl-1,3-thiazolidine-2-thiones using a commercially available nickel(II) complex, (Me3P)2NiCl2, has been developed for tropylium and trityl tetrafluoroborate salts. The reaction provides a single diastereomer of the corresponding adducts in good to high yields, which, in turn, can be easily converted into a wide array of enantiomerically pure compounds that are difficult to obtain by other asymmetric procedures.

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Current status and future prospects of Marine Natural Products (MNPs) as antimicrobials

The marine environment is a rich source of chemically diverse, biologically active natural products, and serves as an invaluable resource in the ongoing search for novel antimicrobial compounds. Recent advances in extraction and isolation techniques, and in state-of-the-art technologies involved in organic synthesis and chemical structure elucidation, have accelerated the numbers of antimicrobial molecules originating from the ocean moving into clinical trials. The chemical diversity associated with these marine-derived molecules is immense, varying from simple linear peptides and fatty acids to complex alkaloids, terpenes and polyketides, etc. Such an array of structurally distinct molecules performs functionally diverse biological activities against many pathogenic bacteria and fungi, making marine-derived natural products valuable commodities, particularly in the current age of antimicrobial resistance. In this review, we have highlighted several marine-derived natural products (and their synthetic derivatives), which have gained recognition as effective antimicrobial agents over the past five years (2012?2017). These natural products have been categorized based on their chemical structures and the structure-activity mediated relationships of some of these bioactive molecules have been discussed. Finally, we have provided an insight into how genome mining efforts are likely to expedite the discovery of novel antimicrobial compounds.

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Kinase profiling in early stage drug discovery: Sorting things out

Protein kinases represent one of the largest superfamilies of drugable targets and a major research area for both the pharmaceutical industry and academic groups. This has resulted in the emergence of numerous screening technologies and services dedicated to kinase profiling. In spite of this plentiful offering, the field is not without its own pitfalls, as the profusion of reported conditions and data can ultimately complicate interpretation of project results. Here, we discuss how kinase profiling was used in our early stage drug discovery efforts, from the perspective of a smaller biotech relying largely on assay outsourcing.

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