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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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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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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. Safety of (S)-4-Isopropylthiazolidine-2-thione, C6H11NS2. A document type is Article, introducing its new discovery., Safety of (S)-4-Isopropylthiazolidine-2-thione

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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More research is needed about 1,1-Dioxo-isothiazolidine

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POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC M2 RECEPTOR

The present application relates to positive allosteric modulators of the muscarinic M2 receptor, especially to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular disorders and/or renal disorders.

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Synthesis, characterization and acute anti-inflammatory evaluation of new mefenamic acid derivatives having 4-thiazolidinone nucleus

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug’s potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, COA of Formula: C3H5NOS, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2682-49-7

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Chemistry of 4-Hydroxy-2(1H)-quinolone. Part 1: Synthesis and reactions

This review summarizes results from the literature concerning the synthesis and chemical reactivity of 4-hydroxy-2(1H)-quinolone as well as its reactions that are reported. Most imaginable reaction types have been successfully applied and used, as many of the synthetized compounds exhibit interesting biological activity in various fields.

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One-step synthesis of 2-thiazolidinone

An efficient and direct access to thiazolidinone is developed. 2-Thiazolidinone is synthesized by urea and 2-Aminoethylmercaptan hydrochloride and this one-step process proceeds with good yields, under mild conditions. The structure of the compound was confirmed by IR, 1H NMR, MS and the product purity was 98 % by HPLC.

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Phosphine Organocatalysis

The hallmark of nucleophilic phosphine catalysis is the initial nucleophilic addition of a phosphine to an electrophilic starting material, producing a reactive zwitterionic intermediate, generally under mild conditions. In this Review, we classify nucleophilic phosphine catalysis reactions in terms of their electrophilic components. In the majority of cases, these electrophiles possess carbon-carbon multiple bonds: alkenes (section 2), allenes (section 3), alkynes (section 4), and Morita-Baylis-Hillman (MBH) alcohol derivatives (MBHADs; section 5). Within each of these sections, the reactions are compiled based on the nature of the second starting material – nucleophiles, dinucleophiles, electrophiles, and electrophile-nucleophiles. Nucleophilic phosphine catalysis reactions that occur via the initial addition to starting materials that do not possess carbon-carbon multiple bonds are collated in section 6. Although not catalytic in the phosphine, the formation of ylides through the nucleophilic addition of phosphines to carbon-carbon multiple bond-containing compounds is intimately related to the catalysis and is discussed in section 7. Finally, section 8 compiles miscellaneous topics, including annulations of the Hueisgen zwitterion, phosphine-mediated reductions, iminophosphorane organocatalysis, and catalytic variants of classical phosphine oxide-generating reactions.

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