Category: Triazoles

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, Drug Metabolism and Disposition called The disposition of voriconazole in mouse, rat, rabbit, guinea pig, dog, and human, Author is Roffey, S. J.; Cole, S.; Comby, P.; Gibson, D.; Jezequel, S. G.; Nedderman, A. N. R.; Smith, D. A.; Walker, D. K.; Wood, N., which mentions a compound: 86404-63-9, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3O, Application In Synthesis of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Voriconazole is a new triazole antifungal agent with potent, wide-spectrum activity. Its pharmacokinetics and metabolism have been studied in mouse, rat, rabbit, dog, guinea pig, and humans after single and multiple administration by both oral and i.v. routes. Absorption of voriconazole is essentially complete in all species. The elimination of voriconazole is characterized by non-linear pharmacokinetics in all species. Consequently, pharmacokinetic parameters are dependent upon dose, and a superproportional increase in area under the curve is seen with increasing dose in rat and dog toxicol. studies. Following multiple administration, there is a decrease in systemic exposure. This is most pronounced in mouse and rat, less so in dog, and not observed in guinea pig or rabbit. Repeat-dose toxicol. studies in mouse, rat, and dog have demonstrated that induction of cytochrome P 450 by voriconazole (autoinduction of metabolism) is responsible for the decreased exposure in these species. Autoinduction of metabolism is not observed in humans, and plasma steady-state concentrations remain constant with time. Voriconazole is extensively metabolized in all species. The major pathways in humans involve fluoropyrimidine N-oxidation, fluoropyrimidine hydroxylation, and Me hydroxylation. Also, N-oxidation facilitates cleavage of the mol., resulting in loss of the fluoropyrimidine moiety and subsequent conjugation with glucuronic acid. Major pathways are represented in animal species. The major circulating metabolite in rat, dog, and human is the N-oxide of voriconazole. It is not thought to contribute to efficacy since it is at least 100-fold less potent than voriconazole against fungal pathogens in vitro.

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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: 562074-59-3, is researched, Molecular C7H5ClN2, about Symmetry-based ligand design and evaluation of small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 interaction, the main research direction is immune checkpoint inhibitor surface plasmon resonance PD1 PDL1; Drug design; Immune checkpoint inhibitor; PD-1; PD-L1; Small-molecules; Surface plasmon resonance.Recommanded Product: 562074-59-3.

The development of small mol. inhibitors of PD-1/PD-L1 is eagerly anticipated for treatment of cancer. We focused on the symmetry of the ternary complex structure of reported small mol. ligands and hPD-L1 homodimers, and designed partially- or fully-sym. compounds for more potent inhibitors. The design of the new compounds was guided by our hypothesis that the designed sym. compound would induce a flip of sidechain of ATyr56 protein residue to form a new cavity. The designed compound 4 exhibited substantially increased binding affinity to hPD-L1, as well as PD-1/PD-L1 inhibitory activity in physiol. conditions. Compound 4 also showed a dose-dependent increase in IFN-γ secretion levels in a mixed lymphocyte reaction assay. These results not only indicate the feasibility of targeting the PD-1/PD-L1 pathway with small mols., but illustrate the applicability of the symmetry-based ligand design as an attractive methodol. for targeting protein-protein interaction stabilizers.

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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 Intramolecular Diaza-Diels-Alder Protocol: A New Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks.Formula: C10H9BrN2S.

Phenotype-based screening of diverse compound collections generated by privileged substructure-based diversity-oriented synthesis (pDOS) is considered one of the prominent approaches in the discovery of novel drug leads. However, one key challenge that remains is the development of efficient and modular synthetic routes toward the facile access of privileged small-mol. libraries with skeletal and stereochem. complexity and drug-like properties. In this regard, a novel and diverse one-pot procedure for the diastereoselective synthesis of privileged polycyclic benzopyrans and benzoxepines is described herein. These unexplored chemotypes were accessed by utilizing an acid-mediated diaza-Diels-Alder reaction of 2-allyloxy- and/or homoallyloxy benzaldehyde with 2-aminoazine building blocks. Profiling of representative analogs against blood-stage Plasmodium falciparum parasites identified three lead candidates with low micromolar antimalarial activity.

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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: 3222-47-7, is researched, SMILESS is O=C(O)C1=CN=C(C)C=C1, Molecular C7H7NO2Journal, Article, ACS Medicinal Chemistry Letters called Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists, Author is Nakajima, Ryota; Oono, Hiroyuki; Sugiyama, Sakae; Matsueda, Yohei; Ida, Tomohide; Kakuda, Shinji; Hirata, Jun; Baba, Atsushi; Makino, Akito; Matsuyama, Ryo; White, Ryan D.; Wurz, Ryan Ρ.; Shin, Youngsook; Min, Xiaoshan; Guzman-Perez, Angel; Wang, Zhulun; Symons, Antony; Singh, Sanjay K.; Mothe, Srinivasa Reddy; Belyakov, Sergei; Chakrabarti, Anjan; Shuto, Satoshi, the main research direction is nuclear receptor RORyt triazolopyridine inverse agonist SAR pharmacokinetics.Application In Synthesis of 6-Methylnicotinic acid.

The retinoic acid receptor-related orphan nuclear receptor γt (RORγt), a promising therapeutic target, is a major transcription factor of genes related to psoriasis pathogenesis such as interleukin (IL)-17A, IL-22, and IL-23R. On the basis of the X-ray cocrystal structure of RORγt with 1a, an analog of the known piperazine RORγt inverse agonist 1, triazolopyridine derivatives of 1 were designed and synthesized, and analog 3a was found to be a potent RORγt inverse agonist. Structure-activity relationship studies on 3a, focusing on the treatment of its metabolically unstable cyclopentyl ring and the central piperazine core, led to a novel analog, namely, 6-methyl-N-(7-methyl-8-(((2S,4S)-2-methyl-1-(4,4,4-trifluoro-3-(trifluoromethyl)butanoyl)piperidin-4-yl)oxy)[1,2,4]triazolo[1,5-a]pyridin-6-yl)nicotinamide (5a), which exhibited strong RORγt inhibitory activity and a favorable pharmacokinetic profile. Moreover, the in vitro and in vivo evaluation of 5a in a human whole-blood assay and a mouse IL-18/23-induced cytokine expression model revealed its robust and dose-dependent inhibitory effect on IL-17A production

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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.Sheng, Chun Quan; Zhang, Wan Nian; Ji, Hai Tao; Song, Yun Long; Zhang, Min; Zhou, You Jun; Lu, Jia Guo; Zhu, Jue researched the compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ).Formula: C10H7F2N3O.They published the article 《Design, synthesis and antifungal activity of novel triazole derivatives》 about this compound( cas:86404-63-9 ) in Chinese Chemical Letters. Keywords: chloroacetophenone reaction triazole; triazolyl acetophenone preparation epoxidation; oxirane triazolylmethyl difluorophenyl preparation reaction piperazine derivative; triazole diflurophenyl piperazinyl hydroxypropyl derivative preparation antifungal activity. We’ll tell you more about this compound (cas: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.

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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: 86404-63-9, is researched, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3OJournal, Article, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues, Author is Aher, Nilkanth G.; Pore, Vandana S.; Mishra, Nripendra N.; Kumar, Awanit; Shukla, Praveen K.; Sharma, Aanchal; Bhat, Manoj K., the main research direction is triazole containing fluconazole analog preparation antifungal.Recommanded Product: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

Fluconazole based mimics containing 1,2,3-triazole were designed and synthesized as antifungal agents. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Three compounds were found to be more potent against Candida fungal pathogens than control drugs fluconazole and amphotericin B. The studies presented here provide structural modification of fluconazole to give 1,2,3-triazole containing mols. Furthermore, these mols. were evaluated in vivo against Candida albicans i.v. challenge in Swiss mice and antiproliferative activities were tested against human hepatocellular carcinoma Hep3B and human epithelial carcinoma A431. It was found that compound I resulted in 97.4% reduction in fungal load in mice and did not show any profound proliferative effect at lower dose (0.001 mg/mL).

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

Recommanded Product: 3222-47-7. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 6-Methylnicotinic acid, is researched, Molecular C7H7NO2, CAS is 3222-47-7, about Versatile {Cp2Ti} Grafted Hetero-Polyoxotungstate Clusters: Synthesis, Crystal Structure, and Photocurrent Properties. Author is Singh, Vikram; Liu, Shuang; Ma, Pengtao; Drew, Michael G. B.; Wang, Jingping; Niu, Jingyang.

Polyoxotungstate supported titanocene {Cp2Ti}2+ clusters H6{K8(Cp2Ti)2P4W24O88(PO4)2}·14H2O (1), H6[Na2P4W14O58(Cp2Ti)2]·12H2O (2), and H2[K6{Cp2Ti}{PW9O33(WO2)}2{NC5H3(COOK)2}(NC5H3(CH3)COOK)·22H2O] (3) have been synthesized, and their single crystal x-ray structures have revealed unprecedented and intriguing structural features. The synthesized compounds have been characterized by various spectroscopic techniques including UV-vis, cyclic voltammogram, NMR, ESI-MS, and inductive coupled plasma spectroscopy (ICP) in solution and also by IR, TGA, and diffuse reflectance in the solid state. Clusters 1 and 2 are rare examples of lacunary POM supported titanocene clusters obtained by incorporating various phosphorus heteroatoms to form elusive phosphotungstate assemblies, whereas 3 is an unprecedented organometallic as well as heteroleptic pyridyl functionalized POM. Clusters 1-3 show transient photocurrent ON/OFF behavior upon UV-light irradiation and also exhibit characteristic TiIV/III intravalence electron transfer. This behavior is also established by their cyclic voltammograms in mixed phosphate buffers (Na2HPO4/NaH2PO4) which show the evidence of POM supported {Cp2Ti}2+/+ species in their redox solution Furthermore, ESR line broadening is also observed in these clusters at room temperature, a fact which also confirms the formation of partially reduced/oxidized {Cp2Ti}2+/+ species leading to TiIV/III intravalence electron transfers within all three clusters. The {Cp2Ti}2+ decorated polyoxometalate cluster 3 shows improved transient photocurrent behavior which may be due to the presence of pyridyl carboxyl ions which provide better surface contact for the cluster mol. through the carboxylate moiety to the ITO electrode.

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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, Huaxi Yaoxue Zazhi called Synthesis of fluconazole, Author is Wang, Jianxiang, which mentions a compound: 86404-63-9, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3O, Name: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone.

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

Safety of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone. 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 of novel substituted tetrazoles having antifungal activity. Author is Upadhayaya, Ram Shankar; Jain, Sanjay; Sinha, Neelima; Kishore, Nawal; Chandra, Ramesh; Arora, Sudershan K..

In an effort to find potent antifungal agents, a variety of triazole derivatives with a 5-substituted tetrazole structure, e.g., I, were prepared and evaluated for antifungal activity against Candida spp., Cryptococcus neoformans, and Aspergillus spp. in vitro. The location of the Me group at the C-3 of of two of the series has been demonstrated to be a key structural element of antifungal potency.

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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 Particle beam-mass spectrometric analysis of difluorophenyl triazole compounds using normal phase-HPLC. Author is Creaser, Colin S.; Stygall, James W.; Bowen, David V.; Pullen, Frank S..

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