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, Research Support, Non-U.S. Gov’t, European Journal of Medicinal Chemistry called New azoles with potent antifungal activity: Design, synthesis and molecular docking, Author is Che, Xiaoying; Sheng, Chunquan; Wang, Wenya; Cao, Yongbing; Xu, Yulan; Ji, Haitao; Dong, Guoqiang; Miao, Zhenyuan; Yao, Jianzhong; Zhang, Wannian, which mentions a compound: 86404-63-9, SMILESS is FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1, Molecular C10H7F2N3O, Product Details of 86404-63-9.

In response to the urgent need for novel antifungal agents with improved activity and broader spectrum, computer modeling was used for rational design of novel antifungal azoles. On the basis of the active site of lanosterol 14α-demethylase from Candida albicans (CACYP51), a series of new azoles with substituted-phenoxypropyl piperazine side chains were rationally designed and synthesized. In vitro antifungal activity assay indicates that the new azoles show good activity against most of the tested pathogenic fungi. Interestingly, the designed compounds are also active against an azole-resistant clin. strain. Compared to fluconazole and itraconazole, several compounds (such as I) show higher antifungal activity and a broader spectrum, which are promising leads for the development of novel antifungal agents.

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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, RSC Medicinal Chemistry called Design and optimisation of a small-molecule TLR2/4 antagonist for anti-tumour therapy, Author is Xu, Qun; Li, Tian; Chen, Hekai; Kong, Jun; Zhang, Liwei; Yin, Hang, the main research direction is nitrovinyl arene preparation antitumor SAR.Computed Properties of C7H7NO2.

A small-mol. co-inhibitor that targets the TLR2/4 signalling pathway were developed. After high-throughput screening of a compound library containing 14400 small mols., followed by hit-to-lead structural optimization, the compound I was finally obtained, which has effective inhibitory properties against the TLR2/4 signalling pathways. This compound was found to significantly inhibit multiple pro-inflammatory cytokines released by RAW264.7 cells. This was followed by compound I demonstrating promising efficacy in subsequent anti-tumor experiments The current results provided a novel understanding of the role of TLR2/4 in cancer and a novel strategy for anti-tumor therapy.

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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, 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., the main research direction is voriconazole antifungal metabolite toxicokinetic pharmacokinetic species difference.Category: triazoles.

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

Related Products of 86404-63-9. 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 triazole antifungal derivatives by heterocycle-benzene bioisosteric replacement. Author is Jiang, Zhigan; Wang, Yan; Wang, Wenya; Wang, Shengzheng; Xu, Bo; Fan, Guorong; Dong, Guoqiang; Liu, Yang; Yao, Jianzhong; Miao, Zhenyuan; Zhang, Wannian; Sheng, Chunquan.

On the basis of the authors’ previously discovered triazole antifungal lead compounds, heterocycle-benzene bioisosteric replacement was used to improve their pharmacokinetic profile. The designed new triazole derivatives have good antifungal activity toward a wide range of pathogenic fungi. Their binding mode with the target enzyme was clarified by mol. docking. The MIC value of the highly potent compound 1-(4-(benzo[d]thiazol-2-yl-methyl)piperazin-1-yl)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol against Candida albicans, Candida tropicalis, and Cryptococcus neoformans is 0.016 μg/mL, 0.004 μg/mL, and 0.016 μg/mL, resp. Moreover, preliminary pharmacokinetic studies revealed that it showed improved oral absorption as compared to the lead compound iodiconazole and deserved for further evaluations.

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

Reference of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone. 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 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. Author is Lebouvier, Nicolas; Giraud, Francis; Corbin, Typhanie; Na, Young Min; Le Baut, Guillaume; Marchand, Pascal; Le Borgne, Marc.

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

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 Sequencing [4+1]-Cycloaddition and Aza-Michael Addition Reactions: A Diastereoselective Cascade for the Rapid Access of Pyrido[2′,1′:2,3]/Thiazolo[2′,3′:2,3]imidazo[1,5-a]quinolone Scaffolds as Potential Antibacterial and Anticancer Motifs, published in 2019-11-15, which mentions a compound: 65705-44-4, Name is 4-(4-Bromophenyl)-5-methylthiazol-2-amine, Molecular C10H9BrN2S, Recommanded Product: 65705-44-4.

The design and synthesis of a quality compound library containing a small number of skeletally diverse scaffolds, whose members rapidly deliver new chem. probes active against multiple phenotypes, is paramount in drug discovery. In this context, an efficient one-pot strategy for the synthesis of a mini library of sp3 enriched hexahydropyrido[2′,1′:2,3]imidazo[1,5-a]quinolinium and hexahydrothiazolo[2′,3′:2,3] imidazo[1,5-a]quinolinium architectures, is described. This new one-pot method features a combination of Sc(OTf)3-catalyzed [4+1]-cycloaddition with aza-Michael addition reactions.The cascade results in a rapid and diastereoselective formation of these scaffolds via desymmetrization of the oxidative-dearomatization products of phenols. Phenotypic screening of the mini library against multidrug resistant bacteria and a panel of cancer cell lines identified potential antibacterial and anticancer lead drug candidates.Further investigation of the anticancer leads, indicated their activity as tubulin-polymerization inhibitors, representing a promising approach for cancer therapy.

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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 Novel alkylated azoles as potent antifungals. Author is Shrestha, Sanjib K.; Garzan, Atefeh; Garneau-Tsodikova, Sylvie.

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. In addition to the literature in the link below, there is a lot of literature about this compound(1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone)Safety of 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, illustrating the importance and wide applicability of this compound(86404-63-9).

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: 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, the main research direction is benzoxazepinium fuse imidazopyridine preparation; thiazoimidazobenzooxazepinium trifluoromethane sulfonate preparation; pyridothiazoimidazooxzazepinoquinolium trifluoromethane sulfonate preparation; imidazopyrazinoimidazothiazole preparation.SDS of cas: 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.

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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.Robinson, Donovan J.; Spurlin, Sean P.; Gorden, John D.; Karimov, Rashad R. researched the compound: 6-Methylnicotinic acid( cas:3222-47-7 ).Computed Properties of C7H7NO2.They published the article 《Enantioselective Synthesis of Dihydropyridines Containing Quaternary Stereocenters Through Dearomatization of Pyridinium Salts》 about this compound( cas:3222-47-7 ) in ACS Catalysis. Keywords: dihydropyridine piperidine preparation enantioselective; pyridinium salt dearomatization rhodium BINAP catalyst. We’ll tell you more about this compound (cas:3222-47-7).

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

Recommanded Product: 188781-36-4. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Chloro-6-methylpyrazine-2-carboxylic acid, is researched, Molecular C6H5ClN2O2, CAS is 188781-36-4, about MPX-004 and MPX-007: new pharmacological tools to study the physiology of nmda receptors containing the GluN2A subunit. Author is Volkmann, Robert A.; Fanger, Christopher M.; Anderson, David R.; Sirivolu, Venkata Ramana; Paschetto, Kathy; Gordon, Earl; Virginio, Caterina; Gleyzes, Melanie; Buisson, Bruno; Steidl, Esther; Mierau, Susanna B.; Fagiolini, Michela; Menniti, Frank S..

GluN2A is the most abundant of the GluN2 NMDA receptor subunits in the mammalian CNS. Physiol. and genetic evidence implicate GluN2A-containing receptors in susceptibility to autism, schizophrenia, childhood epilepsy and neurodevelopmental disorders such as Rett Syndrome. However, GluN2A-selective pharmacol. probes to explore the therapeutic potential of targeting these receptors have been lacking. Here we disclose a novel series of pyrazine-containing GluN2A antagonists exemplified byMPX-004 (5-(((3-chloro-4-fluorophenyl) sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl)pyrazine-2-carboxamide) and MPX- 007 (5-(((3-fluoro-4-fluorophenyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl) methylpyrazine-2-carboxamide). MPX-004 and MPX-007 inhibit GluN2A-containing NMDA receptors expressed in HEK cells with IC50s of 79 nM and 27 nM, resp. In contrast, at concentrations that completely inhibited GluN2A activity these compounds have no inhibitory effect on GluN2B or GluN2D receptor-mediated responses in similar HEK cell-based assays. Potency and selectivity were confirmed in electrophysiol. assays in Xenopus oocytes expressing GluN2A-D receptor subtypes. Maximal concentrations of MPX-004 and MPX-007 inhibited ∼30%of the whole-cell current in rat pyramidal neurons in primary culture and MPX- 004 inhibited ∼60% of the total NMDA receptor-mediated EPSP in rat hippocampal slices. GluN2A-selectivity at native receptors was confirmed by the finding that MPX-004 had no inhibitory effect on NMDA receptor mediated synaptic currents in cortical slices from GRIN2A knock out mice. Thus, MPX-004 and MPX-007 offer highly selective pharmacol. tools to probe GluN2A physiol. and involvement in neuropsychiatric and developmental disorders.

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