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Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists

Antagonists of the corticotropin-releasing factor (CRF) neuropeptide should prove to be effective in treating stress and anxiety-related disorders. In an effort to identify antagonists with improved physicochemical properties, new tricyclic CRF1 antagonists were designed, synthesized, and tested for biological activity. As a result of studies aimed at establishing a relationship between structure and CRF1 binding affinity, NBI 35965 (12a) was identified as a high-affinity antagonist with a pKi value of 8.5. Compound 12a proved to be a functional CRF1 antagonist with pIC50 values of 7.1 and 6.9 in the in vitro CRF-stimulated cAMP accumulation and ACTH production assays, respectively, and 12a also reduced CRF or stress induced ACTH production in vivo.

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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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QUINUCLIDINE DERIVATIVES AS MUSCARINIC M3 RECEPTOR ANTAGONISTS

The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for? the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.

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

Discovery of 6-Bromobenzo[d]isoxazol-3(2H)-one

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 65685-51-0. In my other articles, you can also check out more blogs about 65685-51-0

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Chromatography-free, Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids to 3-hydroxybenzisoxazoles

The Mitsunobu reaction has become one of the most powerful tools to alkylate acidic pronucleophiles. A significant caveat of Mitsunobu chemistry, however, is that the reaction mixture is often plagued with purification problems owing to the phosphine oxide and hydrazine dicarboxylate by-products. In addition to the development of more readily separable Mitsunobu reagents, the product’s physicochemical properties may be exploited to facilitate purification. In this regard, we present a swift and efficient preparation of 3-hydroxybenzisoxazoles by the Mitsunobu-triggered heterocyclizations of salicylhydroxamic acids, which can be isolated by an acid?base work-up. As expected, a range of functional groups was compatible with the chemistry.

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

Awesome Chemistry Experiments For 21725-69-9

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Electric Literature of 21725-69-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.21725-69-9, Name is Benzo[d]isoxazol-3-ol, molecular formula is C7H5NO2. In a Article£¬once mentioned of 21725-69-9

Synthesis of 3-(1,2-benzisoxazolin-3-on-2-yl)-propionic acids derivatives

In the reaction of 3-hydroxy-1,2-benzisoxazole and its 5-chloro- and 6-chloro- derivatives with 3-bromopropionic acid only N-substituted products were obtained. Esters and amides of these acids and N-dibenzylaminomethyl- and N-hydroxymethylamides were synthetized.

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

Extracurricular laboratory:new discovery of 3-Chloro-1,2-benzisoxazole

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METHODS OF USING PIPERIDYL-BENZISOXAZOLE AND BENISOTHIAZOLE DERIVATIVES AS CHOLINESTERASE INHIBITORS

Disclosed herein are compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer’s disease

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

Can You Really Do Chemisty Experiments About Benzo[d]isoxazol-3-ol

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Process for the preparation of 6-(perfluoroalkyl) uracil compounds from 2-(N,N-disubstituted) amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds

An improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula I STR1 from 2-(N,N-disubstituted)amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds having the structural formula II STR2

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

The important role of 3,5-Dichlorobenzo[d]isoxazole

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 16263-53-9 is helpful to your research. Related Products of 16263-53-9

Related Products of 16263-53-9, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 16263-53-9, molcular formula is C7H3Cl2NO, introducing its new discovery.

1,2-benzoisoxazole derivative or its salt and brain-protecting agent comprising the same

This invention relates to a 1,2-benzoisoxazole derivative represented by the following general formula (I) or its salt: STR1

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

Final Thoughts on Chemistry for Benzo[d]isoxazol-3-ol

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SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR IDENTIFICATION, DESIGN AND USE

Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.

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

Discovery of 3-Methyl-1,2-benzisoxazol-6-ol

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 66033-92-9, and how the biochemistry of the body works.category: Benzisoxazole

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 66033-92-9, name is 3-Methyl-1,2-benzisoxazol-6-ol, introducing its new discovery. category: Benzisoxazole

Synthesis of Oxazolo<5,4-g>-1,2-benzisoxazoles

Several oxazolo<5,4-g>-1,2-benzisoxazoles have been synthesised starting from 7-amino-6-hydroxy-3-methyl-1,2-benzisoxazole (II) following two methods.The first method involves cyclization of the schiff bases (III) obtained from II and aromatic aldehydes using N-bromosuccinimide, and in the second method cyclocondensation of II with aromatic acids is brought about in the presence of polyphosphoric acid.The title isoxazoles form a new class of heterocyclic compounds.

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

Final Thoughts on Chemistry for 21725-69-9

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Computed Properties of C7H5NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 21725-69-9, in my other articles.

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Amyloid binding nitrogen-linked compounds for the antemortem diagnosis of alzheimer’s disease, in vivo imaging and prevention of amyloid deposits

Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer’s brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down’s Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

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