Discovery of 2-(Chloromethyl)benzo[d]oxazole

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 41014-43-1 is helpful to your research. Related Products of 41014-43-1

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SYNTHESIS OF 2-(4-ARYL-1E,3E-BUTADIENYL)BENZOXAZOLES BY THE HORNER-WADSWORTH-EMMONS REACTION

2-(4-Aryl-1E,3E-butadienyl)benzoxazole derivatives were synthesized by the Horner-Wadsworth-Emmons reaction of 2-phosphorylmethylbenzoxazoles with cinnamaldehydes in fair to good yield.

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STORE OVERLOAD-INDUCED CALCIUM RELEASE INHIBITORS AND METHODS FOR PRODUCING AND USING THE SAME

The present invention provides compounds having store overload-induced Ca2+ release (SOICR) inhibitory activity and methods for producing and using the same. In particular, compounds of the invention is of the formula: R1-X1-L-X2-R2, wherein R1, X1, L, X2, and R2 are those defined herein.

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Benzoxazole – Wikipedia,
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Samarium diiodide mediated barbier-type reaction of 2-chloromethylbenzoxazole and 2-chloromethylbenzothiazole with carbonyl compounds: A convenient synthesis of 1-(beta-hydroxyalkyl)benzoxazoles and 1-(beta-hydroxyalkyl)benzothiazoles

1-(beta-Hydroxyalkyl)benzoxazoles and 1-(beta -hydroxyalkyl)benzothiazoles were prepared via reductive addition reactions of 2-chloromethylbenzoxazole and 2-chloromethylbenzothiazole with carbonyl compounds under mild conditions mediated by SmI2.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Discovery of 41014-43-1

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Synthesis and reactivity of halogeno-difluoromethyl aromatics and heterocycles: Application to the synthesis of gem-difluorinated bioactive compounds

In an effort to prepare new fluorine-containing compounds which are active against HIV, and based on the electrochemical reduction of a series of bromodifluoromethyl compounds, the tetrakis(dimethylamino)ethylene (TDAE) was found to be an effective reductant of the 2-(bromodifluoromethyl)benzoxazole 1 and of the 5-(bromodifluoromethyl)-3-phenyl-1,2,4-oxadiazole 3. A stepwise electron transfer with a difluoromethyl radical as intermediate is assumed to take place in this reaction. Under mild conditions, the generated difluoromethyl heterocyclic anion was efficiently trapped with aromatic and heterocyclic aldehydes 7-14 and ketones 15-16. In this way the corresponding beta,beta-difluoro-alpha-heteroarylated alcohols 17-32 were obtained in moderate to good yields. The same methodology was successfully applied to the reduction of chlorodifluoromethylated ketones 4-6 and the generated alpha,alpha-difluoroacetyl anion was trapped with several aldehydes 7, 8, 10, 11, under mild conditions, to give the corresponding 2,2-difluoro-3-hydroxy ketone derivatives 33-38, in moderate yields. The SRN1 reactions of 2-(bromodifluoromethyl)benzoxazole (1) with the anions of heterocyclic thiols and phenolic compounds were also carried out. The products 39-54, which all have a CF2 group, were tested for activity against HIV, and several were found to be active, including 44 which was very active.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis and characterization of the ligand based on benzoxazole and its transition metal complexes: DNA-binding and antitumor activity

A new ligand 2-((2-((benzo[d]oxazol-2-yl)methoxy)phenoxy)methyl)benzoxazole (L) and its four transition metal complexes M(NO3)2L (M=Cu, Co, Ni, Zn), have been synthesized and investigated. The single crystal structures of the complexes show that all of them have similar molecular structure and the ligand exhibits good coplanarity after coordination with the metal ions. Further investigation of DNA binding indicates that both the ligand L and the complexes can bond to DNA by intercalation mode, and the latter possesses much stronger binding affinity. Antitumor activity of these compounds tested on the four cancer cell lines, follows the order: Cu-L>Ni-L?Co-L>Zn-L?L, which are thought to be related with their DNA-binding affinity.

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Benzoxazole – Wikipedia,
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Synthetic Route of 41014-43-1, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 41014-43-1, Name is 2-(Chloromethyl)benzo[d]oxazole, molecular formula is C8H6ClNO. In a Article£¬once mentioned of 41014-43-1

Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors

A novel series of heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids was studied as leukotriene biosynthesis inhibitors. A hypothesis of structure-activity optimization by insertion of an oxime moiety was investigated using REV-5901 as a starting point. A systematic structure- activity optimization showed that the spatial arrangement and stereochemistry of the oxime insertion unit proved to be important for inhibitory activity. The promising lead, S-(E)-11, inhibited LTB4 biosynthesis in the intact human neutrophil with IC50 of 8 nM and had superior oral activity in vivo, in a rat pleurisy model (ED50 = 0.14 mg/kg) and rat anaphylaxis model (ED50 = 0.13 mg/kg). In a model of lung inflammation, S-(E)-11 blocked LTE4 biosynthesis (ED50 of 0.1 mg/kg) and eosinophil influx (ED50 of 0.2 mg/kg). S-(E)-11 (A-93178) was selected for further preclinical evaluation.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 41014-43-1, and how the biochemistry of the body works.Formula: C8H6ClNO

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, 41014-43-1, name is 2-(Chloromethyl)benzo[d]oxazole, introducing its new discovery. Formula: C8H6ClNO

Indoles via Knoevenagel-Hemetsberger reaction sequence

A series of substituted indoles have been synthesized by the sequential reaction of aromatic aldehydes with ethyl azidoacetate in the presence of sodium ethoxide to form the corresponding ethyl alpha-azido-beta-arylacrylates (Knoevenagel process) followed by a solvent mediated thermolysis (Hemetsberger process). The isolated yields of the ethyl alpha-azido-beta-arylacrylates were significantly increased when employing the sacrificial electrophile ethyl trifluoroacetate. 1H NMR and coupled 1H-13C NMR analysis of the ethyl alpha-azido-beta-arylacrylates indicate that the condensation is stereospecific – only the Z-isomer could be detected. Solvent mediated thermal treatment of the meta-substituted ethyl alpha-azido-beta- arylacrylates resulted in the formation of both the 5- and 7- substituted indoles – the 5-regioisomer being slightly favored over the 7-regioisomer. Analogous thermal treatment of (2Z, 2Z?)-diethyl 3,3?-(1,3- phenylene)bis(2-azidoacrylate) and (2Z, 2Z?)-diethyl 3,3?-(1,4- phenylene)bis(2-azidoacrylate) exclusively produced pyrroloindoles, diethyl 1,5-dihydropyrrolo[2,3-f]indole-2,6-dicarboxylate and diethyl 1,5-dihydropyrrolo[2,3-f]indole-2,6-dicarboxylate, respectively. Results are also reported which indicate that the alpha-azido-beta-arylacrylates can be used in the subsequent Hemetsberger indolization process without prior purification.

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Benzoxazole – Wikipedia,
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Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents

Tremendous efforts have been dedicated to the development of effective therapeutics against Alzheimer’s disease, which represents the most common debilitating neurodegenerative disease. Multifunctional agents are molecules designed to have simultaneous effects on different pathological processes. Such compounds represent an emerging strategy for the development of effective treatments against Alzheimer’s disease. Here, we report on the synthesis and biological evaluation of a series of nitroxoline-based analogs that were designed by merging the scaffold of 8-hydroxyquinoline with that of a known selective butyrylcholinesterase inhibitor that has promising anti-Alzheimer properties. Most strikingly, compound 8g inhibits self-induced aggregation of the amyloid beta peptide (Abeta1-42), inhibits with sub-micromolar potency butyrylcholinesterase (IC50 = 215 nM), and also selectively complexes Cu2+. Our study thus designates this compound as a promising multifunctional agent for therapeutic treatment of Alzheimer’s disease. The crystal structure of human butyrylcholinesterase in complex with compound 8g is also solved, which suggests ways to further optimize compounds featuring the 8-hydroxyquinoline scaffold.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Creating an antibacterial with in vivo efficacy: Synthesis and characterization of potent inhibitors of the bacterial cell division protein FTSZ with improved pharmaceutical properties

3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.

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Synthesis, antifungal activities and molecular docking studies of benzoxazole and benzothiazole derivatives

Based on benzoxazole and benzothiazole scaffold as an important pharmacophore, two series of 2-(aryloxymethyl) benzoxazole and benzothiazole derivatives were synthesized and their antifungal effects against eight phytopathogenic fungi were evaluated. Compounds 5a, 5b, 5h, and 5i exhibited significant antifungal activities against most of the pathogens tested. Especially 5a, 5b, 5h, 5i, 5j, and 6h inhibited the growth of F. solani with IC50 of 4.34?17.61 mug/mL, which were stronger than that of the positive control, hymexazol (IC50 of 38.92 mug/mL). 5h was the most potent inhibitor (IC50 of 4.34 mug/mL) against F. Solani, which was about nine times more potent than hymexazol. Most of the test compounds displayed significant antifungal effects against B. cinerea (IC50 of 19.92?77.41 mug/mL), among them, 5a was the best one (IC50 of 19.92 mug/mL). The structure-activity relationships (SARs) were compared and analyzed. The result indicates that the electron-drawing ability and position of the substituents have a significant impact on biological activities. Furthermore, docking studies were carried out on the lipid transfer protein sec14p from S. cerevisiae, and preliminarily verified the antifungal activities. Taken together, these results provide 2-(phenoxymethyl)benzo[d]oxazole as an encouraging framework that could lead to the development of potent novel antifungal agents.

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Benzoxazole – Wikipedia,
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