Discovery of Isoquinoline N-Oxide

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Fast regioselective sulfonylation of pyridine/quinoline N-oxides induced by iodine

Fast sulfonylation of pyridine/quinoline N-oxides induced by iodine is demonstrated herein. The regioselective protocol occurs under metal-free conditions in a short reaction time (10 min), exhibiting high efficiency (up to 92% yield) and good compatibility (up to 33 examples). A gram-scale reaction was conducted with only a slight loss of production.

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Simple exploration of Isoquinoline-3-carboxylic acid

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SAR Studies Leading to the Identification of a Novel Series of Metallo-beta-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model

The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-beta-lactamase (MBL) and serine-beta-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new beta-lactamase inhibitors to be used in conjunction with carbapenems and other beta-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-beta-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem.

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Some scientific research about 486-73-7

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INHIBITORS OF BACE

The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer’s Disease and other BACE-mediated diseases.

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Top Picks: new discover of 1-(Isoquinolin-1-yl)ethanone

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Thiazolyl and benzothiazolyl hydrazones derived from alpha-(N)-acetylpyridines and diazines: Synthesis, antiproliferative activity and CoMFA studies

The synthesis of a series of thiazolyl and benzothiazolyl hydrazones derived from alpha-(A3-acylpyridines, -quinolines, -isoquinolines, -pyridazines, -pyrimidines, and -pyrazines is reported. The stereochemistry of these compounds was determined by NMR spectroscopic methods. The antiproliferative activity of the novel compounds was quantified in tissue culture (melanoma, breast carcinoma, colon adenocarcinoma, epitheloid cervix carcinoma, Burkitt’s lymphoma, leukemia, and hydroxyurea sensitive and resistant myelogenous leukemia sublines). All compounds exhibited profound antiproliferative activity, in particular against Burkitt’s lymphoma cells. Out of this series, compounds 6b, 7b, 7c, 8c and 8i were found to be 13-900 times more potent than hydroxyurea and no cross-resistance to hydroxyurea was observed. A predictive 3D-QSAR model using the CoMFA approach was established.

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Archives for Chemistry Experiments of 3-Methylisoquinoline

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Imidazole and imidazoline derivatives and uses thereof

This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human alpha2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the alpha2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

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Properties and Exciting Facts About 24188-72-5

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5-Nitrofuran-2-ylmethyl group as a potential bioreductively activated pro-drug system

5-Substituted isoquinolin-1-ones have been synthesised by one-pot Curtius rearrangement of the corresponding substituted 3-phenylpropenoyl azides and cyclisation. Arylmethylation of the anions of the isoquinolinones with benzyl halides [4-methoxybenzyl chloride, 2-(chloromethyl)furan and 5-nitro-2-(tosyloxymethyl)furan] takes place exclusively at nitrogen. Nitration of 2-(furan-2-ylmethyl)isoquinolin-1-one in strongly acidic medium gives 2-(5-nitrofuran-2-ylmethyl)isoquinolin-1-one, whereas weaker acidic conditions lead to dinitration. Curtius rearrangement of 3-carboranylbutanoyl azide and trapping with 5-nitrofuran-2-ylmethanol gives 5-nitrofuran-2-ylmethyl N-(3-carboranylpropyl)carbamate. Biomimetic reduction of these nitrofuranylmethyl derivatives of anticancer drugs triggers release of the parent drugs. Thus, these nitrofurans have potential applications as pro-drugs for selective release of therapeutic drugs in hypoxic solid tumours.

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Simple exploration of (1,2,3,4-Tetrahydroisoquinolin-3-yl)methanol

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INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

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Discovery of 7-Bromo-3,4-dihydro-2H-isoquinolin-1-one

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Axial chirality control during suzuki-miyaura cross-coupling reactions: The tert-Butylsulfinyl group as an efficient chiral auxiliary

An efficient route to a new family of axially chiral biaryl ligands by a Suzuki-Miyaura cross-coupling reaction between ortho,ortho’-disubstituted aryl iodides bearing in ortho position a tert-butyl or p-tolylsulfinyl group and ortho-substituted phenyl boronic acids or esters is described. The comparison between the t-BuSO and p-TolSO groups as chiral controllers is reported. The modularity of the approach is demonstrated by the preparation of a variety of enantiopure axially chiral mixed S/N and S/P ligands.

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Extracurricular laboratory:new discovery of 19493-44-8

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One-step Synthesis of 3-(Dialkylamino)indolizines by the Palladium-catalyzed Reaction of alpha-Bromopyridine, Propargyl Alcohol, and Secondary Amine

3-(Dialkylamino)indolizines were synthesized in one step by the reaction of 2-bromopyridine, propargyl alcohol, and secondary amines in the presence of Pd(PPh3)2Cl2-CuI as a catalyst. 3-(2-Pyridyl)-2-propyn-1-ol and 3-(2-pyridyl)acrylaldehyde were suggested to be intermediates of the reaction. 3-Dialkylamino derivatives of pyrrolo<1,2-a>quinoline, pyrrolo<2,1-a>isoquinoline, and pyrrolo<1,2-b>pyridazine were obtained from the corresponding alpha-haloazaaromatics in a similar way.

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Can You Really Do Chemisty Experiments About 6624-49-3

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Non-platinum complexes containing releasable biologically active ligands

Since the discovery of anticancer activity of cisplatin and other transition metal complexes, a lot of compounds have been reported as containing ligand(s) bearing its(their) own biological activity. Nowadays, the complexes containing releasable bioactive ligand(s), for which several terms (e.g., multi-targeted, multi-action or multi-modal) have been introduced, represent one of the hottest topics for the bioinorganic chemists. Herein we focused on rationally designed cytotoxic complexes of platinum-group metals, namely ruthenium, rhodium, palladium, osmium and iridium, which contain releasable bioactive ligand(s). Because a concept of multi-targeted complexes is based on a release and subsequent joint biological effect of multiple species, we concentrate especially on complexes whose fate under the (pseudo)physiological conditions is provably or most likely connected with a release of bioactive ligand(s)/substituent(s) and cytotoxic metal-containing species. Thus, the simultaneous action of the released species ensures various biological profits, such as higher cytotoxic activity, cytotoxicity at different cells (connected with the ability to overcome resistance) or modified processes connected with the mode of action, as compared with the initial complexes without bioactive ligand(s).

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