New explortion of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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N-phenyl-4-pyrazolo[1,5-6]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy

Glycogen synthase kinase 3 regulates glycogen synthase, the rate-determining enzyme for glycogen synthesis. Liver and muscle glycogen synthesis is defective in type 2 diabetics, resulting in elevated plasma glucose levels. Inhibition of GSK-3 could potentially be an effective method to control plasma glucose levels in type 2 diabetics. Structure-activity studies on a N-phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine series have led to the identification of potent and selective compounds with good cellular efficacy. Molecular modeling studies have given insights into the mode of binding of these inhibitors. Since the initial leads were also potent inhibitors of CDK-2/CDK-4, an extensive SAR was performed at various positions of the pyrazolo[1,5-b] pyridazin core to afford potent GSK-3 inhibitors that were highly selective over CDK-2. In addition, these inhibitors also exhibited very good cell efficacy and functional response. A representative example was shown to have good oral exposure levels, extending their utility in an in vivo setting. These inhibitors provide a viable lead series in the discovery of new therapies for the treatment of type 2 diabetes.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. COA of Formula: C8H9NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

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Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators

Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Properties and Exciting Facts About 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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2-AMINOQUINAZOLINE DERIVATIVE

An object of the present invention is to provide compounds which are useful as protein kinase inhibitors.Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I): wherein R1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.An object of the present invention is to provide compounds which are useful as protein kinase inhibitors. Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I): wherein R 1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R 2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R 2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Palladium-catalyzed selective synthesis of 3,4-dihydroquinazolines from electron-rich arylamines, electron-poor arylamines and glyoxalates

A simple palladium-catalyzed selective synthesis of structurally diverse 3,4-dihydroquinazolines from electron-rich arylamines, electron-poor arylamines and glyoxalates has been developed under mild conditions. This reaction is carried out in a tandem manner constituted by the condensation of arylamines and glyoxalates, the selective Diels-Alder cycloaddition and oxidation processes, in which 4-nitrothiophenol was used as the key ligand.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Multi-dimensional target profiling of N,4-diaryl-1,3-thiazole-2-amines as potent inhibitors of eicosanoid metabolism

Eicosanoids like leukotrienes and prostaglandins play a considerable role in inflammation. Produced within the arachidonic acid (AA) cascade, these lipid mediators are involved in the pathogenesis of pain as well as acute and chronic inflammatory diseases like rheumatoid arthritis and asthma. With regard to the lipid cross-talk within the AA pathway, a promising approach for an effective anti-inflammatory therapy is the development of inhibitors targeting more than one enzyme of this cascade. Within this study, thirty N-4-diaryl-1,3-thiazole-2- amine based compounds with different substitution patterns were synthesized and tested in various cell-based assays to investigate their activity and selectivity profile concerning five key enzymes involved in eicosanoid metabolism (5-, 12-, 15-lipoxygenase (LO), cyclooxygenase-1 and -2 (COX-1/-2)). With compound 7, 2-(4-phenyl)thiazol-2-ylamino)phenol (ST-1355), a multi-target ligand targeting all tested enzymes is presented, whereas compound 9, 2-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol (ST-1705), represents a potent and selective 5-LO and COX-2 inhibitor with an IC50 value of 0.9 ¡À 0.2 muM (5-LO) and a residual activity of 9.1 ¡À 1.1% at 10 muM (COX-2 product formation). The promising characteristics and the additional non-cytotoxic profile of both compounds reveal new lead structures for the treatment of eicosanoid-mediated diseases.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Some scientific research about 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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 22013-33-8 is helpful to your research. Synthetic Route of 22013-33-8

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1,2,3-Dithiazoles-new reversible melanin synthesis inhibitors: A chemical genomics study

A chemical genomic screen of an in-house library of small molecule heterocycles was carried out using Xenopus laevis embryos. This led to the identification of N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-4-methoxyaniline (1c), which elicits loss of pigmentation in melanophores and the retinal pigment epithelium (RPE) of developing embryos, independent of the developmental stage of initial exposure. The phenotype was reversible, since pigmentation returned upon compound removal while analysis of neural crest cell markers (Pax7) and melanophore markers (Dct/Xtrp2) revealed that both neural crest precursors and fully differentiated melanophores were present in the dithiazole 1c treated embryos. A subsequent focused structure-activity relationship (SAR) study identified the more active dithiazole 4-benzyloxy-N-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-aniline (1l) and the need for a chlorine substituent at the dithiazole C-4 position. Both the initial chemical genomic screen and the focused SAR study highlighted the toxicity of (dithiazolylidene)aminoazines, and also of methoxyaniline (anisidine) analogues that hosted strong electron-withdrawing or electronegative substituents or acidic hydroxyl groups on the anisidine moiety. This study suggests that 1,2,3-dithiazoles can act as reversible melanin synthesis inhibitors, revealing a new biological activity for this class of compounds. The inhibition of melanin synthesis is medically relevant as a potential treatment for pigmentation disorders such as melasma.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Novel azanaphtoquinone compounds with aromatic amino moiety: Synthesis, structural characterization, and antimicrobial features

New azanaphtoquinone compounds with aromatic moiety were synthesized and their structures were defined by Fourier transform infrared, 13C NMR, 1H NMR and mass spectra. The activities of synthesized azanaphthoquinones as antimicrobial agents against three strains of Gram-positive, four strains of Gram-negative and as well as against three strains of fungi were also investigated. Compound 3d showed eight times greater antibacterial activity against the most sensitive organism being S. epidermidis with a MIC value of 1.22 mug/mL than the reference antimicrobial compound Cefuroxime (MIC = 9.8 mug/mL). For compound 3c, the antibacterial activity against S. epidermidis and S. aureus was equal to that of Cefuroxime and Cefuroxime-Na, respectively. The antibacterial activity of the compounds 3c and 3d were two times stronger against E. faecalis than the reference antimicrobial compound Amikacin. The results obtained in this study revealed that newly synthesized compounds 3c, 3d, and 3e are effective in treating infectious caused by especially Gram-positive bacteria have developed multiple resistances to antibiotics and are favorable structures in designing novel antimicrobial agents.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Cytotoxic small molecule dimers and their inhibitory activity against human breast cancer cells

Small molecules based upon natural product dimers that exhibit cytotoxic activity were synthesized and evaluated for their anti-proliferative activity in human breast cancer cell lines. A central isophthalic core structure linking aromatic amines containing 3,5-disubstitutions produced the most active compounds. This series of compounds was found to be more active against the estrogen receptor positive cell line MCF-7 than the estrogen receptor negative cell line, SKBr3.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 22013-33-8, and how the biochemistry of the body works.Electric Literature of 22013-33-8

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Chlorotrimethylsilane-mediated synthesis of functionalized fused pyridines: Reaction of 3-formylchromones with electron-rich aminoheterocycles

The reaction of 3-formylchromones with aminoheterocycles was investigated. A simple and flexible general procedure for annulation of 5-(2-hydroxybenzoyl) pyridines was proposed. The best reaction conditions were found to be heating the reaction mixture in DMF in the presence of Me3SiCl as a promoter and water as scavenger. Georg Thieme Verlag Stuttgart.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Rapid and convenient synthesis of N-arylmorpholines under microwave irradiation

A series of N-arylmorpholines 1a-1n was obtained by cyclocondensation of arylamines and diethylene glycol dimesylate under microwave irradiation in an aqueous potassium carbonate medium. The reaction is rapid and convenient, and a variety of functional groups are tolerated in the process.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem