Month: March 2022

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 3222-47-7, is researched, SMILESS is O=C(O)C1=CN=C(C)C=C1, Molecular C7H7NO2Journal, Article, European Journal of Medicinal Chemistry called Searching for new agents active against Candida albicans biofilm: A series of indole derivatives, design, synthesis and biological evaluation, Author is Pandolfi, Fabiana; D’Acierno, Federica; Bortolami, Martina; De Vita, Daniela; Gallo, Fabio; De Meo, Alessandra; Di Santo, Roberto; Costi, Roberta; Simonetti, Giovanna; Scipione, Luigi, the main research direction is indole Candida antibiofilm; Candida albicans biofilm; Galleria mellonella; Indole derivatives.Recommanded Product: 3222-47-7.

Candida albicans biofilm represents a major clin. problem due to its intrinsic tolerance to anti-fungal compounds and it has been highly related to infections in catheterized patients. Few compounds are described as able to inhibit biofilm formation or to interfere with preformed biofilm of C. albicans. Here the authors report the in vitro evaluation of anti-biofilm activity on C. albicans ATCC 10231 of a series of new and already known amine and amide indole derivatives Among the studied compounds, fifteen resulted active on C. albicans ATCC 10231 biofilm, with BMIC50 ≤16 μg/mL. Three of them (7, 23 and 33) showed a selectivity towards mature biofilm and the most active of them was the compound 23 (BMIC50 = 4 μg/mL). On the other hands, two different compounds (21 and 22) were selective towards biofilm formation with BMIC50 values of 8 μg/mL. Otherwise, compounds 16 and 17 resulted active on biofilm formation, with BMIC50 of 8 μg/mL and 2 μg/mL resp., and on mature biofilm with BMIC50 of 2 μg/mL. These two last compounds also showed an interesting activity towards the planktonic cells of C. albicans. A selection of the more active compounds was also evaluated on different C. albicans strains (PMC1042, PMC1083 and ATCC 10261), showing a comparable or higher anti-biofilm activity, especially on mature biofilm. In vivo toxicity studies using the Galleria mellonella larvae, were finally carried out on more active indole derivatives, showing that they are poorly toxic even at the highest concentrations tested (500-1000 μg/mL).

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

Quality Control of 6-Methylnicotinic acid. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 6-Methylnicotinic acid, is researched, Molecular C7H7NO2, CAS is 3222-47-7, about Enantioselective Synthesis of Dihydropyridines Containing Quaternary Stereocenters Through Dearomatization of Pyridinium Salts. Author is Robinson, Donovan J.; Spurlin, Sean P.; Gorden, John D.; Karimov, Rashad R..

Enantioselective synthesis of non-aromatic heterocycles containing a quaternary stereogenic center is a challenging synthetic problem. A strategy towards this problem involving dearomatization of N-alkylpyridinium salts using boronic acid nucleophiles have been described. This dearomatization reaction is catalyzed by Rhodium(I)/BINAP catalyst and delivers dihydropyridines that contain a fully substituted stereogenic center alpha to the ring nitrogen atom in high yield and enantioselectivity. The reaction is compatible with a wide range of functional groups such as halide, ester, amide, olefin and free alc. Derivatization of dehydropyridine products allows synthesis of the functionalized tetrahydropyridines and piperidines.

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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

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

Electric Literature of C10H7F2N3O. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Ethyl 2-{[7-fluoro-4-oxo-3-(1H-1,2,4-triazol-1-yl)-4H-thiochromen-2-yl]sulfanyl}acetate. Author is Li, Yang; Xiao, Tao; Yu, Guang Yan; Liu, Dong Liang.

In the title compound, C15H12FN3O3S2, the two six-membered rings are essentially coplanar, their mean planes making a dihedral angle of 1.1 (2)°. The carbonyl C, the two attached non-fused C atoms and the S atom deviate from the plane of the benzene ring by -0.046 (5), -0.017 (5), 0.000 (6), 0.026 (4) Å, resp. The angle between the mean planes of the triazole ring and the sulfur heterocycle is 53.3 (1)°. In the crystal, intermol. C-H…O hydrogen bonds link the mols. in a stacked arrangement along the a axis. Crystallog. data are given.

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

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 3222-47-7, is researched, Molecular C7H7NO2, about Discovery of quinolone derivatives as antimycobacterial agents, the main research direction is quinolone preparation antimycobacterial.Category: triazoles.

In this report, a compound library was screened and identified compound I with antituberculosis activity and a minimal inhibitory concentration (MIC) against M. tuberculosis of 20μg mL-1. Structure optimization and the structure-activity relationship of 1 as the lead compound enabled the design and synthesis of a series of quinolone derivatives, e.g, II. These compounds were evaluated in vitro for anti-tubercular activity against the M. tuberculosis H37Rv strain. Among them, compounds III [n = 1; R = 3′,5′-dimethoxy-[1,1′-biphenyl], 4-(trifluoromethyl)phenyl, 6-(trifluoromethyl)pyridin-3-yl (IV)] exhibited MIC values in the range of 1.2-3μg mL-1 and showed excellent activity against the tested MDR-TB strain (MIC: 3, 2.9 and 0.9μg mL-1, resp.). All three compounds III were non-toxic toward A549 and Vero cells (>100 and >50μg mL-1, resp.). In addition, an antibacterial spectrum test carried out using compound (IV) showed that this compound specifically inhibits M. tuberculosis. These can serve as a new starting point for the development of anti-TB agents with therapeutic potential.

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

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.Wang, Jianxiang researched the compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ).Quality Control of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.They published the article 《Synthesis of fluconazole》 about this compound( cas:86404-63-9 ) in Huaxi Yaoxue Zazhi. Keywords: fluconazole preparation. We’ll tell you more about this compound (cas:86404-63-9).

The improved synthetic technol. of fluconazole was presented. Fluconazole was produced by 4-step reactions with m-difluorobenzenes as starting material and PEG as phase-transfer catalyst, including acylating with chloroacetyl chloride, substitution reaction with 1,2,4-triazole, the reaction with Me3SOI, and ring opening with 1,2,4-triazole. The product could remove impurity of identical structure after recrystallization, with a yield above 50%. The purity of product was above 98.5%, the quality was stable, and the process is reliable.

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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 Particle beam-mass spectrometric analysis of difluorophenyl triazole compounds using normal phase-HPLC, published in 1997-06-30, which mentions a compound: 86404-63-9, Name is 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, Molecular C10H7F2N3O, COA of Formula: C10H7F2N3O.

Normal phase liquid chromatog. combined with particle beam mass spectrometry has been applied to the anal. of fluconazole, an anti-fungal agent, [2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol] and a related intermediate, UK-51060 [2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)ethan-2-one]. Electron ionization and chem. ionization have been investigated in combination with quadrupole ion trap and magnetic sector mass spectrometers and the spectra obtained compared with those for direct probe anal. A novel method for the introduction of the chem. ionization reagent gas via the interface is described for particle beam-magnetic sector mass spectrometry. Multi-stage scan routines have been implemented on the ion trap for the selective storage of analyte species and removal of solvent ions. Detection limits for both spectrometers have been determined and are discussed in terms of interface geometry and analyte transport characteristics. Normal phase HPLC on silica provided a good separation of the intermediate from the later eluting fluconazole peak.

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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 Direct resolution of a new antifungal agent, voriconazole (UK-109,496) and its potential impurities, by use of coupled achiral-chiral high-performance liquid chromatography, the main research direction is voriconazole resolution HPLC; enantiomer separation voriconazole HPLC.Safety of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Coupled achiral-chiral high-performance liquid chromatog. (HPLC) with an achiral amino-based column coupled with a chiral amylose-based column was used for qual. and quant. determination of the potential chiral and achiral impurities of voriconazole (UK-109,496), a new antifungal agent with two stereogenic centers. The effect of the organic mobile-phase modifier, ethanol, was studied. The assay response was linearly dependent on concentration over the range 1.2-40.4 μg for voriconazole and 2.5-104.0 ng for the impurities. The limit of detection was 2.5 ng for each analyte.

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

Maher, K. published an article about the compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine( cas:65705-44-4,SMILESS:NC1=NC(C2=CC=C(Br)C=C2)=C(C)S1 ).Product Details of 65705-44-4. 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:65705-44-4) through the article.

New 2,3-substituted-1,3-thiazolidin-4-one (6a-f) were prepared by cyclocondensation of 2-[6-(4-chlorobenzyloxy)-2-naphthyliden]-4- (4-substituted phenyl)-5-methyl-1,3-thiazole (5a-f) and mercaptoacetic acid in benzene. The synthesized compounds were characterized on the basis of elemental anal., 1H NMR, 13C NMR and FT-IR. The prepared compounds have been screened in vitro against two Gram- pos. Staphylococcus aureus, Staphylococcus epidermidis, and two Gram-neg. Escherichia coli, Pseudomonas aernuginosa for antibacterial activity and two fungal strains Candida albicans, Candida krusei for antifungal activity using ciprofloxacin, ampicillin and ketoconazole with minimal inhibitory concentration (MIC) value of 10 mcg/L in DMSO. Compounds 6a and 6d showed good antibacterial and antifungal activities compared to reference medications utilized within this study.

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