Category: Triazoles

Application of 86404-63-9. 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: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Novel alkylated azoles as potent antifungals.

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. The article 《Novel alkylated azoles as potent antifungals》 also mentions many details about this compound(86404-63-9)Application of 86404-63-9, you can pay attention to it or contacet with the author([email protected]) to get more information.

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 Functionalisation of esters via 1,3-chelation using NaOtBu: mechanistic investigations and synthetic applications, published in 2021, which mentions a compound: 3222-47-7, mainly applied to ester transesterification deesterification chelation mechanistic synthetic application, Safety of 6-Methylnicotinic acid.

For the first time, both 1,3-chelation and the formation of a tetrahedral intermediate were confirmed as the key factors for the unusual nucleophilic behavior of a metal t-butoxide in a transesterification reaction. NMR and real-time IR spectroscopies and deuterium-labeling experiments were used for the mechanistic investigation. Based on a pivotal point in the mechanistic understanding of the action of t-butoxide anion, several uncovering reactions such as direct access to value-added chiral α-amino acid t-Bu ester with almost complete retention of optical purity via elaborative transesterification, non-hydrolytic deesterification of esters, and selective bond cleavage of 3-benzoyloxazolidin-2-ones, were successfully achieved.

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

Tao, Xiao; Yuan, Lin; Zhang, Xiao-Qing; Jing, Chen; Wang, Jin-Tang 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 ).Synthetic Route of 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 mol. of 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, C10H7F2N3O, the dihedral angle between the planar rings is 84.00(4)°. Intermol. C-H···N H bonds link the mols. and may be effective in stabilizing the crystal structure. Crystallog. data are given.

The article 《1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone》 also mentions many details about this compound(86404-63-9)Synthetic Route of C10H7F2N3O, you can pay attention to it, because details determine success or failure

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

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about ‘Online’ liquid chromatography/nuclear magnetic resonance mass spectrometry – a powerful spectroscopic tool for the analysis of mixtures of pharmaceutical interest.Reference of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Liquid chromatog. (LC), simultaneously coupled with both NMR and mass spectrometry (MS) ‘online’ is a powerful structural tool and has a potentially vast range of uses within the pharmaceutical industry. Data from a mixture of fluconazole and related triazoles were obtained from an LC/NMR-MS system developed ‘inhouse’, demonstrating the power of this novel anal. approach.

The article 《’Online’ liquid chromatography/nuclear magnetic resonance mass spectrometry – a powerful spectroscopic tool for the analysis of mixtures of pharmaceutical interest》 also mentions many details about this compound(86404-63-9)Reference of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, you can pay attention to it, because details determine success or failure

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 Design, synthesis and antifungal activity of novel triazole derivatives, published in 2004-04-30, which mentions a compound: 86404-63-9, mainly applied to chloroacetophenone reaction triazole; triazolyl acetophenone preparation epoxidation; oxirane triazolylmethyl difluorophenyl preparation reaction piperazine derivative; triazole diflurophenyl piperazinyl hydroxypropyl derivative preparation antifungal activity, Product Details of 86404-63-9.

Twenty-one 1-(1H-1,2,4-triazolyl)-2-(2,4-diflurophenyl)-3-(4-substituted-1-piperazinyl)-2-propanol derivatives were designed and synthesized, on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the target compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

The article 《Design, synthesis and antifungal activity of novel triazole derivatives》 also mentions many details about this compound(86404-63-9)Product Details of 86404-63-9, you can pay attention to it, because details determine success or failure

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, Research Support, N.I.H., Extramural, Journal of Biological Chemistry called The small molecule GAT1508 activates brain-specific GIRK1/2 channel heteromers and facilitates conditioned fear extinction in rodents, Author is Xu, Yu; Cantwell, Lucas; Molosh, Andrei I.; Plant, Leigh D.; Gazgalis, Dimitris; Fitz, Stephanie D.; Dustrude, Erik T.; Yang, Yuchen; Kawano, Takeharu; Garai, Sumanta; Noujaim, Sami F.; Shekhar, Anantha; Logothetis, Diomedes E.; Thakur, Ganesh A., which mentions a compound: 3222-47-7, SMILESS is O=C(O)C1=CN=C(C)C=C1, Molecular C7H7NO2, HPLC of Formula: 3222-47-7.

G-protein- gated inwardly-rectifying K+ (GIRK) channels are targets of Gi/o-protein-signaling systems that inhibit cell excitability. GIRK channels exist as homotetramers (GIRK2 and GIRK4) or heterotetramers with nonfunctional homomeric subunits (GIRK1 and GIRK3). Although they have been implicated in multiple conditions, the lack of selective GIRK drugs that discriminate among the different GIRK channel subtypes has hampered investigations into their precise physiol. relevance and therapeutic potential. Here, we report on a highly-specific, potent, and efficacious activator of brain GIRK1/2 channels. Using a chem. screen and electrophysiol. assays, we found that this activator, the bromothiophene-substituted small mol. GAT1508, is specific for brain-expressed GIRK1/2 channels rather than for cardiac GIRK1/4 channels. Computational models predicted a GAT1508- binding site validated by exptl. mutagenesis experiments, providing insights into how urea-based compounds engage distant GIRK1 residues required for channel activation. Furthermore, we provide computational and exptl. evidence that GAT1508 is an allosteric modulator of channel-phosphatidylinositol 4,5-bisphosphate interactions. Through brain-slice electrophysiol., we show that subthreshold GAT1508 concentrations directly stimulate GIRK currents in the basolateral amygdala (BLA) and potentiate baclofen-induced currents. Of note, GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder. In summary, our findings indicate that the small mol. GAT1508 has high specificity for brain GIRK1/2 channel subunits, directly or allosterically activates GIRK1/2 channels in the BLA, and facilitates fear extinction in a rodent model.

The article 《The small molecule GAT1508 activates brain-specific GIRK1/2 channel heteromers and facilitates conditioned fear extinction in rodents》 also mentions many details about this compound(3222-47-7)HPLC of Formula: 3222-47-7, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]) to get more information.

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

COA of Formula: C10H7F2N3O. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single 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 2-Bromo-2-(5-bromo-1H-1,2,4-triazol-1-yl)-1-(2,4-difluorophenyl)ethanone. Author is Wan, Kun; Fang, Bo; Wang, Guang Zhou; Zhou, Cheng He.

In the title compound, C10H5Br2F2N3O, the mean planes of the benzene and triazole rings form a dihedral angle of 84.86 (2)°. In the crystal structure, weak intermol. C-H…O hydrogen bonds link mols. into extended chains propagating along the c axis. Crystallog. data are given.

After consulting a lot of data, we found that this compound(86404-63-9)COA of Formula: C10H7F2N3O can be used in many types of reactions. And in most cases, this compound has more advantages.

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

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: 562074-59-3, is researched, SMILESS is N#CC1=CN=CC(CCl)=C1, Molecular C7H5ClN2Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo, Author is Guo, Jialin; Luo, Longlong; Wang, Zhihong; Hu, Naijing; Wang, Wei; Xie, Fei; Liang, Erguang; Yan, Xinlin; Xiao, Junhai; Li, Song, the main research direction is linear aliphatic amine linked triaryl preparation; programmed cell death 1 ligand SAR antitumor pharmacokinetics.Product Details of 562074-59-3.

A series of novel linear aliphatic amine-linked triaryl derivatives as inhibitors of PD-1/PD-L1 were designed, synthesized, and evaluated in vitro and in vivo. In this chem. series, compound I showed the most potent inhibitory activity and binding affinity with hPD-L1, with an IC50 value of 12 nM and a KD value of 16.2 pM, showing a binding potency approx. 2000-fold that of hPD-1. Compound I could bind with hPD-L1 on the cellular surface and competitively block the interaction of hPD-1 with hPD-L1. In a T cell function assay, I restored the T cell function, leading to increased IFN-γ secretion. Moreover, in a humanized mouse model, compound I significantly inhibited tumor growth without obvious toxicity and showed moderate PK properties after i.v. injection. These results indicated that I is a promising lead for further development of small-mol. PD-1/PD-L1 inhibitors for cancer therapy.

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

Category: triazoles. 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 Discovery of highly potent novel antifungal azoles by structure-based rational design. Author is Wang, Wenya; Sheng, Chunquan; Che, Xiaoying; Ji, Haitao; Cao, Yongbing; Miao, Zhenyuan; Yao, Jianzhong; Zhang, Wannian.

On the basis of the active site of lanosterol 14α-demethylase from Candida albicans (CACYP51), a series of new azoles were designed and synthesized. All the new azoles show excellent in vitro activity against most of the tested pathogenic fungi, which represent a class of promising leads for the development of novel antifungal agents. The MIC80 value of compounds 8c, 8i and 8n against C. albicans is 0.001 μg/mL, indicating that these compounds are more potent than fluconazole, itraconazole and voriconazole. Flexible mol. docking was used to analyze the structure-activity relationships (SARs) of the compounds The designed compounds interact with CACYP51 through hydrophobic, van der Waals and hydrogen-bonding interactions.

After consulting a lot of data, we found that this compound(86404-63-9)Category: triazoles can be used in many types of reactions. And in most cases, this compound has more advantages.

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

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Sequencing Groebke-Blackburn-Bienayme and Aza-Michael Addition Reactions: A Modular Strategy for Accessing a Diverse Collection of Constrained Benzoxazepine and Imidazopyrazine Systems.HPLC of Formula: 65705-44-4.

A divergent strategy that permitted the access to diversely functionalized benzoxazepinium scaffolds fused to various heterocycles was reported. The described strategy featured a one-pot combination of the Groebke-Blackburn-Bienaym reaction and an aza-Michael addition Me (E)-4-(2-formylphenoxy)but-2-enoates were utilized as central elements in this cascade. These building blocks were reacted with a variety of functionalized amino-azines and tert-Bu isocyanide under ytterbium triflate [Yb(OTf)3] catalysis. The cascade represented a rapid, modular and atom-economic process that leaded to the construction of a diverse collection of constrained benzoxazepinium systems from a wide substrate scope.

After consulting a lot of data, we found that this compound(65705-44-4)HPLC of Formula: 65705-44-4 can be used in many types of reactions. And in most cases, this compound has more advantages.

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