Tag: M.W:200-300

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Shrestha, Sanjib K.; Garzan, Atefeh; Garneau-Tsodikova, Sylvie researched the compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ).Category: triazoles.They published the article 《Novel alkylated azoles as potent antifungals》 about this compound( cas:86404-63-9 ) in European Journal of Medicinal Chemistry. Keywords: triazole preparation antifungal; Cytotoxicity; Ergosterol; Fluconazole; Hemolysis; Time-kill curves. We’ll tell you more about this compound (cas:86404-63-9).

The synthesis of new FLC derivatives I (R = 2,4-Cl2, 2-F, 3-F, 4-F, etc.; n = 0, 1, 2, 3, 4, 5) along with their antifungal activity against a panel of 13 clin. relevant fungal strains was developed. Also, their toxicity against mammalian cells, their hemolytic activity, as well as their mechanism of action were explored. Overall, many of our FLC derivatives I exhibited broad-spectrum antifungal activity and all compounds displayed an MIC value of <0.03 μg/mL against at least one of the fungal strains tested. Also, they were found to be less hemolytic and less cytotoxic to mammalian cells than the FDA approved antifungal agent amphotericin B. The mechanism of action of compounds has been demonstrated as best derivative for the inhibition of the sterol 14α-demethylase enzyme, involved in ergosterol biosynthesis. Here is a brief introduction to this compound(86404-63-9)Category: triazoles, if you want to know about other compounds related to this compound(86404-63-9), you can read my other articles.

Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents, published in 2018-01-11, which mentions a compound: 86404-63-9, Name is 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, Molecular C10H7F2N3O, Application of 86404-63-9.

The extensive use of fluconazole (FLC) and other azole drugs has caused the emergence and rise of azole-resistant fungi. The fungistatic nature of FLC in combination with toxicity concerns have resulted in an increased demand for new azole antifungal agents. Herein, we report the synthesis and antifungal activity of novel alkylated piperazines and alkylated piperazine-azole hybrids, their time-kill studies, their hemolytic activity against murine erythrocytes, as well as their cytotoxicity against mammalian cells. Many of these mols. exhibited broad-spectrum activity against all tested fungal strains, with excellent min. inhibitory concentration (MIC) values against non-albicans Candida and Aspergillus strains. The most promising compounds were found to be less hemolytic than the FDA-approved antifungal agent voriconazole (VOR). Finally, we demonstrate that the synthetic alkylated piperazine-azole hybrids do not function by fungal membrane disruption, but instead by disruption of the ergosterol biosynthetic pathway via inhibition of the 14α-demethylase enzyme present in fungal cells.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Recommanded Product: 4-(4-Bromophenyl)-5-methylthiazol-2-amine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.

With the aim to discover orally active small mols. that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl-phthalazinone acetamide (7114863; I) increased glucose uptake (EC50 of 0.07±0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, I was superior to rosiglitazone under similar exptl. conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents, the main research direction is alkylated piperazine azole hybrid synthesis antifungal.Application In Synthesis of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

The extensive use of fluconazole (FLC) and other azole drugs has caused the emergence and rise of azole-resistant fungi. The fungistatic nature of FLC in combination with toxicity concerns have resulted in an increased demand for new azole antifungal agents. Herein, we report the synthesis and antifungal activity of novel alkylated piperazines and alkylated piperazine-azole hybrids, their time-kill studies, their hemolytic activity against murine erythrocytes, as well as their cytotoxicity against mammalian cells. Many of these mols. exhibited broad-spectrum activity against all tested fungal strains, with excellent min. inhibitory concentration (MIC) values against non-albicans Candida and Aspergillus strains. The most promising compounds were found to be less hemolytic than the FDA-approved antifungal agent voriconazole (VOR). Finally, we demonstrate that the synthetic alkylated piperazine-azole hybrids do not function by fungal membrane disruption, but instead by disruption of the ergosterol biosynthetic pathway via inhibition of the 14α-demethylase enzyme present in fungal cells.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ) is researched.Related Products of 86404-63-9.Lebouvier, Nicolas; Giraud, Francis; Corbin, Typhanie; Na, Young Min; Le Baut, Guillaume; Marchand, Pascal; Le Borgne, Marc published the article 《Efficient microwave-assisted synthesis of 1-(1H-indol-1-yl)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents》 about this compound( cas:86404-63-9 ) in Tetrahedron Letters. Keywords: indolyl triazolylpropanol preparation; chloroacetophenone triazole substitution microwave irradiation; triazolylacetophenone preparation epoxidation microwave irradiation; microwave irradiation substitution Corey Chaykovsky epoxidation mediator; aryl triazolylmethyl oxirane preparation indole ring opening. Let’s learn more about this compound (cas:86404-63-9).

Conazole antifungals, in the series of triazole alcs., e.g., I, have been synthesized by ring opening of corresponding oxiranes, e.g., II. These oxiranes were prepared in high yields by Corey-Chaykovsky reaction under microwave irradiation

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Product Details of 86404-63-9. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Process Development of Voriconazole: A Novel Broad-Spectrum Triazole Antifungal Agent. Author is Butters, Mike; Ebbs, Julie; Green, Stuart P.; MacRae, Julie; Morland, Matthew C.; Murtiashaw, Charles W.; Pettman, Alan J..

In the synthesis of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (voriconazole), the relative stereochem. is set in the addition of a 4-(1-metalloethyl)-5-fluoropyrimidine derivative to 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-ethanone. The diastereocontrol of this reaction has been examined by variation of pyrimidine substitution pattern and by changes in the metalation and reaction conditions. Excellent diastereoselection (12:1) is obtained using an organozinc derivative of 6-(1-bromoethyl)-4-chloro-5-fluoropyrimidine. After removal of the chlorine from the pyrimidine ring, the absolute stereochem. of voriconazole is established via a diastereomeric salt resolution process using (1R)-10-camphorsulfonic acid. Synthetic routes to the pyrimidine partner have also been evaluated. The initial six-step development route from 5-fluorouracil has been superseded by a four-step synthesis involving fluorination of Me 3-oxopentanoate and cyclization with formamidine acetate.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Wen, Qin-Mei; Yin, Ben-Tao; Yan, Cong-Yan; Zhou, Cheng-He published an article about the compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9,SMILESS:FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1 ).Formula: C10H7F2N3O. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:86404-63-9) through the article.

In the title mol., C21H19FN4O, the triazole ring forms dihedral angles of 67.0 (1) and 59.6 (1)° with the Ph and fluoro-substituted benzene rings, resp. The dihedral angle between the Ph ring and the fluoro-substituted benzene ring is 79.1 (1)°. The pyrrolidine ring is in a half-chair conformation. In the crystal, weak C-H···O and C-H···N hydrogen bonds connect mols. into layers parallel to (001). Crystallog. data are given.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanol, published in 2012-02-29, which mentions a compound: 86404-63-9, mainly applied to crystal structure difluorophenyltriazolylethanol; mol structure fluorophenyltriazolylethanol; hydrogen bond difluorophenyltriazolylethanol; triazolylethanol difluorophenyl crystal mol structure, COA of Formula: C10H7F2N3O.

In 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanol, C10H9F2N3O, the dihedral angle between the rings is 22.90(4)°. In the crystal, C-H···F and O-H···N H bonds link the mols. into chains along [010]. Crystallog. data are given.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

SDS of cas: 86404-63-9. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Synthesis and crystallographic characterization of 1-((2-(2,4-difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole. A crucial intermediate for the synthesis of azole antifungal drugs. Author is Patel, Pallav D.; Talele, Tanaji T.; Fronczek, Frank R..

Preparation of 1-((2-(2,4-difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole(I) was accomplished in two steps. 1H-1,2,4-triazole was reacted with 2,4-difluoro-α-chloroacetophenone in presence of K2CO3 in refluxing toluene to provide the compound 2,4-difluoro-α-(1H-1,2,4-triazol-2-yl)acetophenone (II). The compound II was treated with trimethylsulfoxonium iodide in aqueous NaOH and toluene to provide the title oxirane. The compound I, previously isolated as an oil, was crystallized from (DCM/MeOH) and characterized by X-ray crystallog.: triclinic, space group P – 1, a = 7.3225 (15), b = 7.5833 (15), c = 9.856 (2) Å, α = 91.908 (12), β = 100.824 (11), γ = 103.800 (11)°, V = 520.28 (18) Å3, Z = 2. This important intermediate I, normally an oil, was crystallized, and its crystal structure includes a stepped conformation with nearly parallel triazole and Ph rings. Lack of classical hydrogen-bond donors leads to packing dominated by weaker interactions, including C-H…N, C-H…F and F…F contacts.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Scientia Pharmaceutica called A validated stability-indicating liquid chromatographic method for determination of degradation impurities and diastereomers in voriconazole tablets, Author is Shaikh, Kabeer A.; Patil, Ashish T., which mentions a compound: 86404-63-9, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3O, Electric Literature of C10H7F2N3O.

A reversed-phase gradient liquid chromatog. method was developed for the quant. determination of Voriconazole, along with its degradation and diastereomeric impurities in tablet dosage form. Chromatog. separation was achieved on an Inertsil ODS 3V, 150 × 4.6 mm, 5 μm column. The mobile phase consisting of solvent A 0.05 M (M) potassium dihydrogen phosphate (pH 2.5 buffer) and solvent B (mixture of acetonitrile and MeOH in the ratio 90:10 (volume/volume)), was delivered at a flow rate of 1.2 mL min-1 with the detection wavelength at 256 nm. Resolution of Voriconazole and all 5 potential impurities was achieved at > 2.0 for all pairs of compounds The drug was subjected to stress conditions such as oxidative, acid and base hydrolysis, and thermal and photolytic degradation Voriconazole was found to degrade significantly under base hydrolysis stress conditions compared to acid hydrolysis stress conditions. The degradation products were well-resolved from the main peak and its impurities, thus proving the stability-indicating power of the method. The stressed samples were assayed against a reference standard and the mass balance was found to be close to 99.0%. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision, and robustness.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics