Extracurricular laboratory:new discovery of Benzo[d]isoxazol-3-amine

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Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors

A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the lead compound 3 to improve its DMPK profile as well as in vitro potency. We identified the thiazole compound 60j with potent inhibitory activity, high brain permeability, and good bioavailability. Compound 60j showed a potent and dose-dependent anti-nociceptive effect in the acetic acid-induced writhing test in mice.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Can You Really Do Chemisty Experiments About 3-Chloro-6-fluorobenzo[d]isoxazole

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5- And/or 7-substituted pyrazolo-[4,3-b]-pyridines and their use as antiinflammatory agents

Compounds of the formula (I) and pharmaceutically acceptable salts thereof: STR1 wherein: the first of R1 and R2 is hydrogen, C1-4 alkyl or phenyl optionally substituted by one or two substituents selected from halogen, CF3, C1-4 alkoxy or alkyl and the second is SR4 wherein R4 is phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl, or NR5 R6 wherein R5 and R6 are independently selected from hydrogen, C1-6 alkyl, C3-8 cycloalkyl, phenyl or phenyl C1-4 alkyl either of which phenyl moieties may be substituted by one or two substituents selected from halogen, CF3, C1-4 alkoxy or C1-4 alkyl, or R5 and R6 together form C4-6 polymethylene; and R3 is hydrogen, C1-4 alkyl or benzyl and is attached at nitrogen atom 1 or 2, having anti-inflammatory activity, a process for their preparation and their use as pharmaceuticals.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of Benzo[d]isoxazol-3-amine

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BROADSPECTRUM SUBSTITUTED BENZISOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs esters and metabolites thereof. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of 1,2-Benzisoxazole-3-acetic Acid

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Process for the preparation of 1,2-benzisoxazole-3-acetic acid

The present invention provides a process for preparing 1,2-benzisoxazole-3-acetic acid, comprising the step of reacting 4-hydroxy-coumarin with hydroxyl-amine in the presence of a base. The present invention further provides a process for preparing a salt of benzisoxazole methane sulfonic acid, comprising the steps of 1) sulfonating 1,2-benzisoxazole-3-acetic acid using chlorosulfonic acid in a solvent mixture comprising methylene chloride and sodium hydroxide; and 2) isolating the salt of benzisoxazole methane sulfonic acid.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Brief introduction of Benzo[d]isoxazol-3-ol

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FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF, MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Top Picks: new discover of 16263-52-8

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Related Products of 16263-52-8, Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 16263-52-8, Name is 3-Chloro-1,2-benzisoxazole. In a document type is Patent,introducing its new discovery.

TRICYCLIC DELTA-3-PIPERIDINES AS ALPHA2- ANTAGONISTS

The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C 1-6alkanediyl; n is 1 or 2; X 1is–O–,–S–,–S(=O)–or–S(=O) 2–; each R 1is independently hydrogen, halogen, C 1-6alkyl, nitro, hydroxy or C 1-4alkyloxy; D is an optionally substituted mono, bi-or tricyclic nitrogen containing heterocycle, a 2H-benzopyranone, a benzamide, a benzophenone or a phenoxyphenyl having central alpha 2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Brief introduction of Benzo[d]isoxazol-3-amine

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Nanoscale synthesis and affinity ranking

Most drugs are developed through iterative rounds of chemical synthesis and biochemical testing to optimize the affinity of a particular compound for a protein target of therapeutic interest. This process is challenging because candidate molecules must be selected from a chemical space of more than 1060 drug-like possibilities 1, and a single reaction used to synthesize each molecule has more than 107 plausible permutations of catalysts, ligands, additives and other parameters 2 . The merger of a method for high-throughput chemical synthesis with a biochemical assay would facilitate the exploration of this enormous search space and streamline the hunt for new drugs and chemical probes. Miniaturized high-throughput chemical synthesis 3-7 has enabled rapid evaluation of reaction space, but so far the merger of such syntheses with bioassays has been achieved with only low-density reaction arrays, which analyse only a handful of analogues prepared under a single reaction condition 8-13 . High-density chemical synthesis approaches that have been coupled to bioassays, including on-bead 14, on-surface 15, on-DNA 16 and mass-encoding technologies 17, greatly reduce material requirements, but they require the covalent linkage of substrates to a potentially reactive support, must be performed under high dilution and must operate in a mixture format. These reaction attributes limit the application of transition-metal catalysts, which are easily poisoned by the many functional groups present in a complex mixture, and of transformations for which the kinetics require a high concentration of reactant. Here we couple high-throughput nanomole-scale synthesis with a label-free affinity-selection mass spectrometry bioassay. Each reaction is performed at a 0.1-molar concentration in a discrete well to enable transition-metal catalysis while consuming less than 0.05 milligrams of substrate per reaction. The affinity-selection mass spectrometry bioassay is then used to rank the affinity of the reaction products to target proteins, removing the need for time-intensive reaction purification. This method enables the primary synthesis and testing steps that are critical to the invention of protein inhibitors to be performed rapidly and with minimal consumption of starting materials.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Awesome and Easy Science Experiments about Benzo[d]isoxazol-3-ol

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1,2-BENZISOSELENAZOL-3(2H)-ONE AND 1,2-BENZISOTHIAZOL-3(2H)-ONE DERIVATIVES AS BETA-LACTAM ANTIBIOTIC ADJUVANTS

Provided herein are compositions and methods useful in the treatment of beta-lactam antibiotic resistant bacteria.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Bioisosteric investigation of ebselen: Synthesis and in vitro characterization of 1,2-benzisothiazol-3(2H)-one derivatives as potent New Delhi metallo-beta-lactamase inhibitors

Carbapenem-resistant Enterobacteriaceae (CRE) producing New Delhi metallo-beta-lactamase (NDM-1) cause untreatable bacterial infections, posing a significant threat to human health. In the present study, by employing the concept of bioisosteric replacement of the selenium moiety of ebselen, we have designed, synthesized and characterized a small compound library of 2-substituted 1,2-benzisothiazol-3(2H)-one derivatives and related compounds for evaluating their cytotoxicity and synergistic activity in combination with meropenem against the E. coli Tg1 (NDM-1) strain. The most promising compound 3a demonstrated potent synergistic activity against a panel of clinically isolated NDM-1 positive CRE strains with FICI as low as 0.09. Moreover, its IC50 value and inhibition mechanism were also confirmed by using the enzyme inhibition assay and the ESI-MS analysis respectively. Importantly, compound 3a has acceptable toxicity and is not a PAINS. Because of its structural simplicity and potent synergistic activity in combination with meropenem, we propose that compound 3a may be a promising meropenem adjuvant and a new series of such compounds may worth further investigations.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of 36216-80-5

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COMPOUNDS

A compound of formula (I), or a pharmaceutical salt thereof.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics