Tag: M.W:100-200

15112-41-1, Name is Benzo[d]oxazole-5-carboxylic acid, belongs to benzoxazole compound, is a common compound. Formula: C8H5NO3In an article, once mentioned the new application about 15112-41-1.

Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)

The fragment-based identification of two novel and potent biochemical inhibitors of the nicotinamide phosphoribosyltransferase (NAMPT) enzyme is described. These compounds (51 and 63) incorporate an amide moiety derived from 3-aminopyridine, and are thus structurally distinct from other known anti-NAMPT agents. Each exhibits potent inhibition of NAMPT biochemical activity (IC 50 = 19 and 15 nM, respectively) as well as robust antiproliferative properties in A2780 cell culture experiments (IC50 = 121 and 99 nM, respectively). However, additional biological studies indicate that only inhibitor 51 exerts its A2780 cell culture effects via a NAMPT-mediated mechanism. The crystal structures of both 51 and 63 in complex with NAMPT are also independently described.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

22876-22-8, Name is 5-Methylbenzo[d]oxazole-2(3H)-thione, belongs to benzoxazole compound, is a common compound. Computed Properties of C8H7NOSIn an article, once mentioned the new application about 22876-22-8.

Based on 1, 3 – propanedithiol as mercapto source synthesis 2 – oxa (thia) and mercaptobenzothiazole azole compound of preparation method (by machine translation)

The invention belongs to the field of medical and chemical intermediate synthesis, provides a based on 1, 3 – propanedithiol as mercapto source synthesis 2 – oxa (thia) and mercaptobenzothiazole azole compound of preparation method, under protection of inert gas, in dimethyl sulfoxide solvent, the oxa (thia) substituted azole with 1, 3 – propanedithiol in the presence of a alkali 120 – 140 C heating and stirring, reaction 12 – 24 hours later, the reaction is cooled down to room temperature, after the acidification is carried out processing to obtain the product. The invention has the reaction condition is simple, functional group compatibility advantages of better and higher yield; the prepared 2 – mercapto-benzoxazole and 2 – mercaptobenzothiazole compound is an important organic synthetic intermediates, raw material in the chemical industry, pesticide, medicine and other field has a very wide application, has strong practical value and social and economic benefits. (by machine translation)

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

3621-81-6, Name is 2,5-Dichlorobenzooxazole, belongs to benzoxazole compound, is a common compound. Computed Properties of C7H3Cl2NOIn an article, once mentioned the new application about 3621-81-6.

Benzoxazolamines and Benzothiazolamines: Potent, Enantioselective Inhibitors of Leukotriene Biosynthesis with a Novel Mechanism of Action

A series of benzoxazolamine and benzothiazolamine analogs that inhibit leukotriene (LT) biosynthesis are described.The initial lead, (S)-N-(benzothiazol-2-yl)phenylalanine ethyl ester (5a), was discovered in a screening program for inhibition of Ca-ionophore-A23187-induced LTB4 release in human polymorphonuclear leukocytes (IC50 0.23 muM).Through structural modification, it was determined that hydrophobic substituents in the 5-position and replacement of the phenyl ring of phenylalanine with a cyclohexyl group greatly enhance potency.Several ester bioisosteres that retain potency and enantiomeric selectivity are described.Lead optimization culminated in (S)-N-<2-cyclohexyl-1-(2-pyridinyl)ethyl>-5-methyl-2-benzoxazolamine (43b), IC50 0.001 muM.The compounds described are not inhibitors of 5-lipoxygenase but, rather, act at the level of arachidonic acid release.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Application of 15112-41-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 15112-41-1, Benzo[d]oxazole-5-carboxylic acid, introducing its new discovery.

Heterocyclic N-acetonylbenzamides and their use as fungicides

Certain N-acetonylbenzamides and their use as fungicides are disclosed. The N-acetonylbenzamides disclosed contain a heterocyclic ring fused to an aromatic ring. These compounds are particularly effective against phytopathogenic fungi of the class Oomycetes. Also disclosed is a method for controlling phytopathogenic fungi by applying one or more of the heterocyclic N-acetonylbenzamides of the present invention, optionally with one or more additional fungicidal compounds.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 15112-41-1. In my other articles, you can also check out more blogs about 15112-41-1

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 13451-79-1, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 13451-79-1, Name is 5-Fluorobenzo[d]oxazol-2(3H)-one, molecular formula is C7H4FNO2

Discovery of potent IDO1 inhibitors derived from tryptophan using scaffold-hopping and structure-based design approaches

Indoleamine 2,3-dioxygenase 1 (IDO1) is frequently hijacked by tumors to escape the host immune response, and the enzyme is now firmly established as an attractive target for cancer immunotherapy. To identify novel IDO1 inhibitors suitable for drug development, a scaffold-hopping strategy combined with the average electrostatic potentials calculation was ultilized to design novel benzoxazolinone derivatives. Among these, compounds 7e, 7f and 9c exhibited the inhibitory potency in the low micromolar range and displayed negligible level of cytotoxicity against HeLa cells. Treatment with these three compounds promoted the proliferation of T lymphocyte and led to the dramatic decrease of regulatory T cells in the B16F1 cells and naive T cells co-culture system. Subsequent spectroscopic experiments suggested that these benzoxazolinones formed a coordinate bond with the heme iron to stabilize the complex. This study suggested that the benzoxazolinone was an interesting scaffold for discovering novel IDO1 inhibitors, and these compounds are attractive candidates for further development.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Recommanded Product: 13451-79-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 13451-79-1, in my other articles.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Electric Literature of 4570-41-6, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 4570-41-6, Benzo[d]oxazol-2-amine, introducing its new discovery.

Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease where motor neurons in cortex, brain stem, and spinal cord die progressively, resulting in muscle wasting, paralysis, and death. Currently, effective therapies for ALS are lacking; however, identification of pathological TAR DNA-binding protein 43 (TDP-43) as the hallmark lesion in sporadic ALS suggests new therapeutic targets for pharmacological intervention. Pathological TDP-43 phosphorylation appears to drive the onset and progression of ALS and may result from upregulation of the protein kinase CK-1 in affected neurons, resulting in postranslational TDP-43 modification. Consequently, brain penetrant specific CK-1 inhibitors may provide a new therapeutic strategy for treating ALS and other TDP-43 proteinopathies. Using a chemical genetic approach, we report the discovery and further optimization of a number of potent CK-1delta inhibitors. Moreover, these small heterocyclic molecules are able to prevent TDP-43 phosphorylation in cell cultures, to increase Drosophila lifespan by reduction of TDP-43 neurotoxicity, and are predicted to cross the blood-brain barrier. Thus, N-(benzothiazolyl)-2-phenyl-acetamides are valuable drug candidates for further studies and may be a new therapeutic approach for ALS and others pathologies in which TDP-43 is involved.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 4570-41-6. In my other articles, you can also check out more blogs about 4570-41-6

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. SDS of cas: 1750-45-4. Introducing a new discovery about 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

Pharmacokinetics behaviors of l-menthol after inhalation and intravenous injection in rats and its inhibition effects on CYP450 enzymes in rat liver microsomes

1. l-Menthol, as a kind of monocyclic terpene, is widely used in inhalation formulations, food and tobacco. The purpose of this study was to investigate the pharmacokinetic behavior of l-menthol as well as its influence on the activities of cytochrome P450 enzymes. 2. The pharmacokinetic behaviors of l-menthol after inhalation (50 mg/kg) and intravenous injection (10 mg/kg) were investigated. A rat liver microsomal model was adopted to elucidate the inhibitory effect of l-menthol on CYP1A2, CYP2C11, CYP2D1/2, CYP2D4, CYP2E1 and CYP3A1 using phenacetin, tolbutamide, omeprazole, dextromethorphan, chlorzoxazone and testosterone as probe drugs, respectively. 3. The plasma concentration reached the Cmax within 1.0 h (inhalation) and descended with the T1/2 of 8.53 and 6.69 h for inhalation and i.v. administration, respectively. IC50 for inhibition of l-menthol on CYP 450 enzymes were 4.35 muM for 2D4, 8.67 muM for 1A2, 13.02 muM for 3A1, 14.78 muM for 2D1/2, 234.9 muM for 2C11 and 525.4 muM for 2E1, respectively. 4. The results illustrate the pharmacokinetic process of l-menthol in rats and provide information for further rational applications. l-Menthol had moderate inhibitions on CYP2D4 and 1A2, which might affect the disposition of medicines primarily dependent on these pathways.

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.SDS of cas: 1750-45-4, you can also check out more blogs about1750-45-4

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Computed Properties of C8H6ClNO, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 41014-43-1, Name is 2-(Chloromethyl)benzo[d]oxazole, molecular formula is C8H6ClNO

Synthesis and reactivity of 2-chloro-5-(4-phenyl-1H-1,2,3-triazol-1-yl) benzenamine

The nucleophilic reactivity of 2-chloro-5-(4-phenyl-1H-1,2,3-triazol-1-yl) benzenamine 5 was studied with different reagents under ultrasonication.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Computed Properties of C8H6ClNO, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 41014-43-1, in my other articles.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Reference of 638192-65-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 638192-65-1, Benzo[d]oxazole-5-carbaldehyde, introducing its new discovery.

Substituted hydroxy-anilino derivatives of cyclobutene-3,4-diones

The compound of the formula: STR1 wherein R1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, or polyfluoroalkyl; and one of R2, R3 and R4 is hydroxyl and the other two are, independently, H, CN, halogen, alkyl or hydroxyl; or a pharmaceutically acceptable salt thereof, is useful as a smooth muscle relaxant.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 638192-65-1. In my other articles, you can also check out more blogs about 638192-65-1

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Application of 22876-21-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 22876-21-7, Name is 5-Nitrobenzo[d]oxazole-2(3H)-thione,introducing its new discovery.

Synthesis and evaluation of the anticonvulsant activities of 4-(2-(alkylthio)benzo[d]oxazol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-ones

In this study, a novel series of 4-(2-(alkylthio)benzo[d]oxazol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-ones (4a?m) was designed and synthesized. The anticonvulsant activities of these compounds were evaluated by using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. The neurotoxicity of these compounds was evaluated using the rotarod neurotoxicity test. The majority of compounds showed anti-MES activities at 100 or 300 mg/kg. Compound 4g was considered to be the most promising, based on its potency against MES- and PTZ-induced seizures with ED50 values of 23.7 and 18.9 mg/kg, respectively. The TD50 value of 4g was 284.0 mg/kg, which resulted in a higher protective index (PI = TD50/ED50) value than that of carbamazepine and valproate. In an ELISA test, compound 4g significantly increased the gamma-aminobutyric acid (GABA) content in mouse brain. In addition, pretreatment with thiosemicarbazide (an inhibitor of the GABA synthesizing enzyme) significantly decreased the activity of 4g in the MES model, which suggests that the mechanism through which compound 4g elicits its anticonvulsive action is at least in part through increasing the GABA level in the brain.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 22876-21-7, and how the biochemistry of the body works.Application of 22876-21-7

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem