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An efficient, catalyst-free, microwave-assisted approach has been developed for the synthesis of 4-azo-butyenolides derivatives by condensing tetronic acid with various anilines. This approach exhibited good functional group compatibility and produced the desired products in good to excellent yields in just 30?40 min. This approach can be seen as a better alternative to protocols with long reaction times used for the synthesis of these compounds, which are synthons for the obtaining of quinolines.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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We recently identified a peptide-peptoid hybrid, PPS1, which specifically recognized lipid-phosphatidylserine (PS). PPS1 consists of distinct positively charged and hydrophobic residue-containing regions. The PPS1 monomer was inactive, but the dimeric form, PPS1D1, displayed strong cytotoxicity to lung cancer cells compared to normal cells in vitro, and reduced the tumor growth in vivo. The minimum pharmacophore of PPS1D1 showed that the first (methionine) and fourth (N-lysine) residues were not important for PPS1D1 cytotoxic activity. In this study, we further investigated these two residues, in particular the fourth residue that lies between the most important four-residue hydrophobic region and two positively charged residues, to determine whether replacements of these moieties could gain activity improvements or render PPS1D1 totally insensitive for binding recognition. The positively charged fourth residue N-lysine was replaced with substituents having varied physiochemical properties, such as aromatic-hydrophobic, aliphatic-alicyclic, heterocyclic, and negatively charged residues, developing a mini-library of 39 derivatives. The standard 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) colorimetric and/or the calcein AM cell viability assays performed on HCC4017 lung cancer cells indicated that the fourth position of PPS1D1 was insensitive to most changes, except that reversal of the negative charge significantly affected the activity. This observation may be due to the neutralization of the nearby positively charged residue that is essential for binding. In addition, shortening each monomeric sequence by eliminating the methionine at the first position did not affect the activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reaction of 2′-benzylbenzohydrazides with concentrated polyphosphoric acid gave 2,5-diaryl-1,3,4-oxadiazoles and a polybenzyl.Cyclodehydration to phthalazines was not observed.It is inferred from product substitution patterns that CH2-N bond cleavage occurs with polybenzyls forming from the benzyl moiety and oxadiazoles from the benzohydrazide fragment.Other reported reactions which generate benzyl fragments lead to bibenzyl and are considered to involve trapping of the cleavage products within a solvent cage.The observed production of polybenzyls is therefore interpreted in terms of the formation of free benzyl fragments.A tetrahydrophthalazine derivative was produced from the addition of diethyl azodicarboxylate to the photodiene of o-methylbenzophenone, but this could not be converted into a phthalazine.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Acetaldehyde dehydrogenase (AdhE) is a bifunctional acetaldehyde?coenzyme A (CoA) dehydrogenase and alcohol dehydrogenase involved in anaerobic metabolism in gram-negative bacteria. This enzyme was recently found to be a key regulator of the type three secretion (T3S) system in Escherichia coli. AdhE inhibitors can be used as tools to study bacterial virulence and a starting point for discovery of novel antibacterial agents. We developed a robust enzymatic assay, based on the acetaldehyde-CoA dehydrogenase activity of AdhE using both absorption and fluorescence detection models (Z? > 0.7). This assay was used to screen ~11,000 small molecules in 384-well format that resulted in three hits that were confirmed by resynthesis and validation. All three compounds are noncompetitive with respect to acetaldehyde and display a clear dose?response effect with hill slopes of 1?2. These new inhibitors will be used as chemical tools to study the interplay between metabolism and virulence and the role of AdhE in T3S regulation in gram-negative bacteria, and as starting points for the development of novel antibacterial agents.

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Benzodioxan,
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Chiral biphenols catalyze the asymmetric Petasis borono-Mannich allylation of aldehydes and amines through the use of a bench-stable allyldioxaborolane. The reaction proceeds via a two-step, one-pot process and requires 2?8 mole % of 3,3?-Ph2-BINOL as the optimal catalyst. Under microwave heating the reaction affords chiral homoallylic amines in excellent yields (up to 99 %) and high enantioselectivies (er up to 99:1). The catalytic reaction is a true multicomponent condensation reaction whereas both the aldehyde and the amine can possess a wide range of structural and electronic properties. Use of crotyldioxaborolane in the reaction results in stereodivergent products with anti- and syn-diastereomers both in good diastereoselectivities and enantioselectivities from the corresponding E- and Z-borolane stereoisomers.

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Benzodioxan,
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A novel double decarboxylative cross-coupling catalyzed by copper and silver has been developed. This method provides a practical approach for the flexible synthesis of alkenes and alkynes from the readily affordable substrates.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidine has been linked to various arylcarbamates to obtain compounds having affinity for dopamine-D1 and -D2, serotonin 5HT(2A) and alpha1-adrenoceptors. When linkers with restricted flexibility are used, the biological activity is reduced indicating that a bended conformation is needed in this series of bioactive molecules. Compounds with a relatively low D2/5HT(2A) affinity ratio in receptor binding experiments and high affinity for the alpha1-adrenoceptors exhibit a pharmacological profile which suggests a preferential effect on the mesocorticolimbic dopaminergic system and an ‘atypical’ antipsychotic activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ?3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem