Category: 4570-41-6

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Recognition of Artificial Nucleobases by E. coli Purine Nucleoside Phosphorylase versus its Ser90Ala Mutant in the Synthesis of Base-Modified Nucleosides

A wide range of natural purine analogues was used as probe to assess the mechanism of recognition by the wild-type (WT) E. coli purine nucleoside phosphorylase (PNP) versus its Ser90Ala mutant. The results were analyzed from viewpoint of the role of the Ser90 residue and the structural features of the bases. It was found that the Ser90 residue of the PNP 1) plays an important role in the binding and activation of 8-aza-7-deazapurines in the synthesis of their nucleosides, 2) participates in the binding of alpha-D-pentofuranose-1-phosphates at the catalytic site of the PNP, and 3) catalyzes the dephosphorylation of intermediary formed 2-deoxy-alpha-D-ribofuranose-1-phosphate in the trans-2-deoxyribosylation reaction. 5-Aza-7-deazaguanine manifested excellent substrate activity for both enzymes, 8-amino-7-thiaguanine and 2-aminobenzothiazole showed no substrate activity for both enzymes. On the contrary, the 2-amino derivatives of benzimidazole and benzoxazole are substrates and are converted into the N1- and unusual N2-glycosides, respectively. 9-Deaza-5-iodoxanthine showed moderate inhibitory activity of the WT E. coli PNP, whereas 9-deazaxanthine and its 2?-deoxyriboside are weak inhibitors. How does it work? The substrate and inhibitory properties of a wide range of artificial bases for the wild-type E. coli purine nucleoside phosphorylase (PNP) versus its Ser90Ala mutant were studied to evaluate the mechanism of recognition by PNP and the role of various electronic and structural features in this process. The PNP recognized a broad palette of bases consisting of a number of dissimilar fragments determining its ability to interact with the Asp204 and Ser90 residues (see scheme).

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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A Straightforward Access to [14C]- and [13C]-Labeled 2-Aminobenzoxazoles and Benzothiazoles via a KCN Polarity Inversion Strategy

A convenient one-pot synthetic access to 2-aminobenzoxazoles and 2-aminobenzothiazoles has been developed. The protocol uses KCN as starting material and proceeds through an in situ polarity inversion step. This approach provides a new valuable and straightforward entry to carbon-14-radiolabeled pharmaceutically relevant heterocycles and substantially reduces as well the amount of radioactive wastes generated.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Reference of 4570-41-6, 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, 4570-41-6, molcular formula is C7H6N2O, introducing its new discovery.

Azolylthioacetamides as a potent scaffold for the development of metallo-beta-lactamase inhibitors

In an effort to develop new inhibitors of metallo-beta-lactamases (MbetaLs), twenty-eight azolylthioacetamides were synthesized and assayed against MbetaLs. The obtained benzimidazolyl and benzioxazolyl substituted 1?19 specifically inhibited the enzyme ImiS, and 10 was found to be the most potent inhibitor of ImiS with an IC50 value of 15 nM. The nitrobenzimidazolyl substituted 20?28 specifically inhibited NDM-1, with 27 being the most potent inhibitor with an IC50 value of 170 nM. Further studies with 10, 11, and 27 revealed a mixed inhibition mode with competitive and uncompetitive inhibition constants in a similar range as the IC50 values. These inhibitors resulted in a 2?4-fold decrease in imipenem MIC values using E. coli cells producing ImiS or NDM-1. While the source of uncompetitive (possibly allosteric) inhibition remains unclear, docking studies indicate that 10 and 11 may interact orthosterically with Zn2 in the active site of CphA, while 27 could bridge the two Zn(II) ions in the active site of NDM-1 via its nitro group.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Electrochemical intramolecular c-h amination: Synthesis of benzoxazoles and benzothiazoles

A new method for metal-free intramolecular C-H amination has been developed. Electrochemical oxidation of 2-pyrimidyloxybenzenes and 2-pyrimidylthiobenzenes, which can be easily prepared from phenols and thiophenols, respectively, followed by the treatment of the resulting pyrimidinium ions with piperidine gives 2-aminobenzoxazoles and 2-aminobenzothiazoles, respectively.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis of Various 2-Aminobenzoxazoles: The Study of Cyclization and Smiles Rearrangement

This study reports two synthetic approaches leading to 2-aminobenzoxazoles and their N-substituted analogues. Our first synthetic strategy involves a reaction between various o-aminophenols and N-cyano-N-phenyl-p-toluenesulfonamide as a nonhazardous electrophilic cyanating agent in the presence of Lewis acid. The second synthetic approach uses the Smiles rearrangement upon activation of benzoxazole-2-thiol with chloroacetyl chloride. Both developed synthetic protocols are widely applicable, afford the desired aminobenzoxazoles in good to excellent yields, and use nontoxic and inexpensive starting material.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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One-pot synthesis of 1-substituted 1H-1,2,3,4-tetrazoles from 2aminothiazoles using tributylmethylammonium chloride as a catalyst

Reaction between substituted thiazolylamine or oxazolylamine, triethyl orthoformate and sodium azide in the presence of tributylmethylammonium chloride in DMSO furnishes 1-substituted 1H-1,2,3,4-tetrazole in high yield.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Electric Literature of 4570-41-6, 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, 4570-41-6, molcular formula is C7H6N2O, introducing its new discovery.

One Pot Synthesis of 4-Arylbenzoxazolo<3,2-a>-s-triazine-2-thiones

The reaction of 2-aminobenzoxazoles (1a-b) with aroyl isothiocyanates in acetone gave 4-arylbenzoxazolo<3,2-a>-s-triazine-2-thiones (3a-g), aroylthioureas (5a-e) and 2-benzoxazolones (6a-b).A reasonable pathway for the formation of 3, 5 and 6 from 1 has been suggested.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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NOVEL HISTONE DEACETYLASE INHIBITORS AND THEIR USE IN THERAPY

A compound of the formula:(I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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, 4570-41-6, name is Benzo[d]oxazol-2-amine, introducing its new discovery. category: benzoxazole

HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE

Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).

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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, name: Benzo[d]oxazol-2-amine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 4570-41-6, Name is Benzo[d]oxazol-2-amine, molecular formula is C7H6N2O

NOVEL FUSED PYRIMIDINE COMPOUND OR SALT THEREOF

Provided is a novel compound having BTK inhibitory action and a cell proliferation suppressing effect. Also provided is a medicine useful for the prevention and/or treatment of a disease associated with BTK, particularly cancer, based on BTK inhibitory action. A compound represented by formula (I) [wherein R1 to R3, W, A, Y and Z respectively have the meanings as defined in the specification], or a salt thereof is disclosed.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem