Kiran, B. Ravi’s team published research in International Journal of Pharmaceutical Sciences and Research in 2015 | CAS: 65685-50-9

5-Bromobenzo[d]isoxazol-3(2H)-one(cas: 65685-50-9) belongs to benzisoxazole.The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. Reference of 5-Bromobenzo[d]isoxazol-3(2H)-one The unique benzisoxazole scaffold also exhibits an impressive potential as antimicrobial, anticancer, anti-inflammatory, anti-glycation agents and so on.

《Synthesis, evaluation of analgesic and anti-inflammatory activities of substituted 1,2-benzoxazolone and 3-chloro-1,2-benzoxazole derivatives》 was published in International Journal of Pharmaceutical Sciences and Research in 2015. These research results belong to Kiran, B. Ravi; Vijayakumar, G. R.; Bharath, H. S.; Sivakumar, R.; Sindhu, S.; Prakash, M. Shet. Reference of 5-Bromobenzo[d]isoxazol-3(2H)-one The article mentions the following:

Herein method for the synthesis of substituted 1,2-benzoxazolone I [R1 = H, NO2, Br; R2 = H, Me, F; R3 = H, NO2, F] and 3-chloro-1,2-benzoxazole derivatives II [R1 = H, NO2, Br; R2 = H, Me, F; R3 = H, NO2, F] was described. A new scheme was adapted for the construction of 1,2-benzoxazole ring from salicylic acid and its derivatives which leads to the formation of series of methyl-2-hydroxy-5-bromo benzoate, Me 2-hydroxybenzoates and N,2-dihydroxybenzamides substituted title compounds Synthesized compounds were characterized by IR, 1H-NMR and Mass spectral anal. Spectral data confirmed the compounds formation. Final compounds I and II were screened for their in-vivo analgesic activity by acetic acid induced writhing method in rats and anti-inflammatory activity by carrageenan-induced paw edema model. Among the compounds screened compound I [R1, R2, R3 = H] and compound II [R1, R2 = H; R3 = NO2] showed good analgesic activity of about 45% (writhing mean 8.9) and 54% (writhing mean 7.5) inhibition resp. at 5 mg/Kg po dosage. Compounds I [R1 = NO2; R2, R3 = H] and II [R1 = NO2; R2, R3 = H] (both having inhibition edema of 66.1%) showed significant anti-inflammatory activity. Other derivatives exhibited moderate to good analgesic and anti-inflammatory activities. The experimental process involved the reaction of 5-Bromobenzo[d]isoxazol-3(2H)-one(cas: 65685-50-9Reference of 5-Bromobenzo[d]isoxazol-3(2H)-one)

5-Bromobenzo[d]isoxazol-3(2H)-one(cas: 65685-50-9) belongs to benzisoxazole.The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. Reference of 5-Bromobenzo[d]isoxazol-3(2H)-one The unique benzisoxazole scaffold also exhibits an impressive potential as antimicrobial, anticancer, anti-inflammatory, anti-glycation agents and so on.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS

The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.

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Benzisoxazole – Wikipedia,
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Synthesis and biological evaluation of D-amino acid oxidase inhibitors

D-Amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including D-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chlorobenzo[d]isoxazol-3-ol (CBIO) potently inhibited DAAO with an IC50 in the submicromolar range. Oral administration of CBIO in conjunction with D-serine enhanced the plasma and brain levels of D-serine in rats compared to the oral administration of D-serine alone.

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BENZISOXAZOLES

The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R1; Y is absent when X represents -Z-R1 and -(C=O)-R6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR 5-carbonyl-; R1 represents C1-4alkyl, Ar1, Ar1-C1-4a1ky1-, -NR3R4 or -Het1; R2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C1-4alkyloxy or C1-4alkyl; R3 and R4 are each independently selected from hydrogen, Ar3 or C1-4alkyl; R5 represents hydrogen, C1-4alkylcarbonyl- or Ar4-carbonyl-; R6 represents a substituent selected from the group consisting of C1.4alkyl, Ar5, Ar6-C1-4alkyl- or NR7R8; R7 and R8 are each independently selected from hydrogen, Het4 or C1-4alkyl; Het1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl, phenyl, phenyl-C1-4alkyl- and phenyl substituted with one or more halo substituents; Het4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl-, phenyl, phenyl-Cl-4alkyl and phenyl substituted with one or more halo substituents; and Ar1, Ar2, Ar3, Ar4, Ar5 or Ar6 each independently represents phenyl optionally substituted one or where possible two or more substituents selected from halo, nitro, C1-4alkyl, hydroxy or C1-4alkyloxy-.

Application In Synthesis of 5-Bromobenzo[d]isoxazol-3(2H)-one, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about Application In Synthesis of 5-Bromobenzo[d]isoxazol-3(2H)-one

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Benzisoxazole – Wikipedia,
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Isoxazole derivatives

An isoxazole compound having the following formula: wherein R1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson’s disease, depression and Alzheimer’s disease.

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Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.category: Benzisoxazole, you can also check out more blogs aboutcategory: Benzisoxazole

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FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

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Benzo[d]isoxazol-3-ol DAAO inhibitors

Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer”s disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein

  • Z1 is N or CR3;
  • Z2 is N or CR4;
  • Z3is O or S;
  • A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof;
  • R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2;
  • R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl;
  • at least one of R1, R2, R3 and R4 is other than hydrogen; and
  • at least one of Z1 and Z2 is other than N.

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    Benzisoxazole – Wikipedia,
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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: 5-Bromobenzo[d]isoxazol-3(2H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 65685-50-9, Name is 5-Bromobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4BrNO2

BENZISOXAZOLES

The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R1; Y is absent when X represents -Z-R1 and -(C=O)-R6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR 5-carbonyl-; R1 represents C1-4alkyl, Ar1, Ar1-C1-4a1ky1-, -NR3R4 or -Het1; R2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C1-4alkyloxy or C1-4alkyl; R3 and R4 are each independently selected from hydrogen, Ar3 or C1-4alkyl; R5 represents hydrogen, C1-4alkylcarbonyl- or Ar4-carbonyl-; R6 represents a substituent selected from the group consisting of C1.4alkyl, Ar5, Ar6-C1-4alkyl- or NR7R8; R7 and R8 are each independently selected from hydrogen, Het4 or C1-4alkyl; Het1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl, phenyl, phenyl-C1-4alkyl- and phenyl substituted with one or more halo substituents; Het4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl-, phenyl, phenyl-Cl-4alkyl and phenyl substituted with one or more halo substituents; and Ar1, Ar2, Ar3, Ar4, Ar5 or Ar6 each independently represents phenyl optionally substituted one or where possible two or more substituents selected from halo, nitro, C1-4alkyl, hydroxy or C1-4alkyloxy-.

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Synthesis and biological evaluation of D-amino acid oxidase inhibitors

D-Amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including D-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chlorobenzo[d]isoxazol-3-ol (CBIO) potently inhibited DAAO with an IC50 in the submicromolar range. Oral administration of CBIO in conjunction with D-serine enhanced the plasma and brain levels of D-serine in rats compared to the oral administration of D-serine alone.

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Reference£º
Benzisoxazole – Wikipedia,
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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of 5-Bromobenzo[d]isoxazol-3(2H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 65685-50-9, Name is 5-Bromobenzo[d]isoxazol-3(2H)-one, molecular formula is C7H4BrNO2

FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

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