Month: January 2023

Nucleoside analogues for the treatment of animal trypanosomiasis was written by Mabille, Dorien;Ilbeigi, Kayhan;Hendrickx, Sarah;Ungogo, Marzuq A.;Hulpia, Fabian;Lin, Cai;Maes, Louis;de Koning, Harry P.;Van Calenbergh, Serge;Caljon, Guy. And the article was included in International Journal of Parasitology: Drugs and Drug Resistance in 2022.Related Products of 1614-12-6 This article mentions the following:

Animal trypanosomiasis (AT) is a parasitic disease with high socio-economic impact. Given the limited therapeutic options and problems of toxicity and drug resistance, this study assessed redirecting our previously identified antitrypanosomal nucleosides for the treatment of AT. Promising hits were identified with excellent in vitro activity across all important animal trypanosome species. Compound 7, an inosine analog, and our previously described lead compound, 3′-deoxytubercidin (8), showed broad spectrum anti-AT activity, metabolic stability in the target host species and absence of toxicity, but with variable efficacy ranging from limited activity to full cure in mouse models of Trypanosoma congolense and T. vivax infection. Several compounds show promise against T. evansi (surra) and T. equiperdum (dourine). Given the preferred target product profile for a broad-spectrum compound against AT, this study emphasizes the need to include T. vivax in the screening cascade given its divergent susceptibility profile and provides a basis for lead optimization towards such broad spectrum anti-AT compound In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Related Products of 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles consist of a five-membered ring containing three nitrogen atoms and are biologically active, especially as antifungal, antimicrobial and enzyme inhibitors. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Related Products of 1614-12-6

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

A naturally occurring isoform-specific probe for highly selective and sensitive detection of human cytochrome P450 3A5 was written by Wu, Jing-Jing;Cao, Yun-Feng;Feng, Liang;He, Yu-Qi;Hong, James Y.;Dou, Tong-Yi;Wang, Ping;Hao, Da-Cheng;Ge, Guang-Bo;Yang, Ling. And the article was included in Journal of Medicinal Chemistry in 2017.Safety of 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:

Cytochrome P 450 (CYP) 3A5 characterized with polymorphic and extensive expression in multiple tissues is the most important P 450 enzyme among the minor CYP3A isoforms. However, a selective and sensitive probe for CYP3A5 remains unavailable. In this study, we identified and characterized a naturally occurring lignan 12 (schisantherin E) as an isoform-specific probe for selective detection of CYP3A5 activity in complex biol. samples. With thorough characterization including LC-MS and NMR, we found that 12 can be metabolized by CYP3A5 to generate a major metabolite 2-O-demethylated 12. Meanwhile, both reaction phenotyping and chem. inhibition experiments further revealed that CYP3A5 selectively catalyzed the 2-O-demethylation of 12. Specifically, the interactions between the Phe210 residue of CYP3A5 and Me benzoate of 12 might play key roles in 12-O-demethylation, which was revealed by docking simulation and site-directed mutagenesis studies. These findings are beneficial for exploring the role of CYP3A5 in drug metabolism and pathol. process. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Safety of 1H-Benzo[d][1,2,3]triazol-1-amine).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to azides. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules.Safety of 1H-Benzo[d][1,2,3]triazol-1-amine

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

Two complexes based on 1H-1,2,3-triazole-4,5-dicarboxylic acid: hydrothermal synthesis, crystal structures and spectral properties was written by Tong, Xiao-Lan;Xin, Jian-Hua;Guo, Wei-Hua;Zhu, Xia-Ping. And the article was included in Journal of Coordination Chemistry in 2011.Product Details of 4546-95-6 This article mentions the following:

[Zn₃(tda)₂(bipy)₂(H₂O)₂·4H₂O]_n (1) and [Co₂(Htda)₂(H₂O)₆·5H₂O] (2) were synthesized and characterized structurally by x-ray diffraction, where H₃tda = 1H-1,2,3-triazole-4, 5-dicarboxylic acid and 2,2′-bipy = 2,2′-bipyridine. Their solid-state structures were characterized by elemental anal. and IR spectroscopy. The mol. unit of 1 consists of two crystallog. unique Zn(II) ions assuming different coordination geometries, the tda^3- exhibits a hexadentate binding mode chelating three Zn(II) ions; neighboring Zn-Zn distances through tda^3- bridges are 5.910(6), 5.888(5), and 6.279(3) Å, resp. In 2, two neighboring Co(II) ions are bridged by two Htda^2- ligands, forming a binuclear structure, with Co-Co distance of 4.091 Å and is further linked to generate a 3-dimensional structure via hydrogen bonds. Fluorescent of 1 was investigated. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6Product Details of 4546-95-6).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.Product Details of 4546-95-6

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

An improved water-soluble/stereospecific biotransformation of aporphine alkaloids in Stephania epigaea to 4R-hydroxyaporphine alkaloids by Clonostachys rogersoniana was written by Cai, Le;Dong, Jian-Wei;Zhao, Li-Xing;Zhou, Hao;Xing, Yun;Li, Ying;Li, Zhen-Jie;Duan, Wei-He;Li, Xue-Jiao;Ding, Zhong-Tao. And the article was included in Process Biochemistry (Oxford, United Kingdom) in 2016.Name: 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:

Aporphine alkaloids were transformed into the corresponding stereospecific 4R-hydroxyaporphine alkaloids through the solid-state fermentation of Stephania epigaea with Clonostachys rogersoniana. This process was validated by both solid- and liquid-state fermentations with aporphine alkaloids as substrates. Cytochrome P 450 enzymes were confirmed to participate in the catalysis of this biotransformation. 4R-Hydroxyaporphine alkaloids exhibit the same levels of acetylcholinesterase (AChE) inhibitory and cytotoxic activities as aporphine alkaloids and are considerably more water soluble than aporphine alkaloids, indicating their potential as water-soluble AChE inhibitors and antitumor agents. This paper suggests that C. rogersoniana fermentation can facilitate a novel biotransformation of aporphine alkaloids in S. epigaea to 4R-hydroxyaporphine alkaloids. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Name: 1H-Benzo[d][1,2,3]triazol-1-amine).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The triazole ring is a relatively stable functional group, and the triazole bond can be used for a variety of applications, such as replacing the phosphate backbone of DNA.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.Name: 1H-Benzo[d][1,2,3]triazol-1-amine

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

3D geometrically frustrated magnets assembled by transition metal ion and 1,2,3-triazole-4,5-dicarboxylate as triangular nodes was written by Zhang, Wei-Xiong;Xue, Wei;Lin, Jian-Bin;Zheng, Yan-Zhen;Chen, Xiao-Ming. And the article was included in CrystEngComm in 2008.Recommanded Product: 1H-1,2,3-Triazole-4,5-dicarboxylic acid This article mentions the following:

Three new chiral metal-organic frameworks, (H₂NMe₂)[M(tzdc)]·0.5H₂O [M=Co(II) (1), Mn(II) (2)] and (NH₄)[Mn(tzdc)]·2.6H₂O (3) (tzdc^3- = 1,2,3-triazole-4,5-dicarboxylate), have been solvothermally synthesized. In the frameworks of 1-3, the ratio of metal and tzdc^3- is 1: 1. Each metal ion is chelated by three tzdc^3- ligands, and each tzdc^3- connects three metal ions, resulting in three-dimensional, 3-connected anionic frameworks, 1 and 2 are isomorphous, and both crystallize in the cubic space group P2₁3. With the template of H₂NMe₂⁺ cations, the frameworks of 1 and 2 have a well-known, porous (10,3)-a network. In contrast, 3 can be obtained by replacing the H₂NMe₂⁺ with smaller NH₄⁺ cations, which leads to a significant topol. change to a unique uniform etd (8,3) network as well as the change of the space group to P6₁. Magnetic studies show dominated antiferromagnetic interactions in 1-3 with θ = -46.8(1), -22.3(1) and -25.8(1) K for 1, 2 and 3, resp. Due to the triangular arrangement of the metal centers, geometrically spin-frustrated magnetism is a characteristic behavior of 1-3. For 1, spin-glassy behavior with a freezing temperature T_f of 2.4 K was distinctly observed, and an empirical factor f = |θ|/T_f ≈ 20 > 10 indicates strong spin-frustration effect. For both 2 and 3, no obvious long-range magnetic ordering and/or spin-glassy behavior was observed down to 2.0 K, which might indicate the f values in them being also larger than 10. By contrast, the observed spin-glassy behavior above 2.0 K in 1 is probably due to the stronger magnetic anisotropy of Co(II) ion and the stronger antiferromagnetic interactions in 1. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6Recommanded Product: 1H-1,2,3-Triazole-4,5-dicarboxylic acid).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Recommanded Product: 1H-1,2,3-Triazole-4,5-dicarboxylic acid

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

5-((3-Amidobenzyl)oxy)nicotinamides as Sirtuin 2 Inhibitors was written by Ai, Teng;Wilson, Daniel J.;More, Swati S.;Xie, Jiashu;Chen, Liqiang. And the article was included in Journal of Medicinal Chemistry in 2016.Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid This article mentions the following:

Derived from the previously reported human sirtuin 2 (SIRT2) inhibitors that were based on a 5-aminonaphthalen-1-yloxy nicotinamide core structure, 5-((3-amidobenzyl)oxy)nicotinamides offered excellent activity against SIRT2 and high isoenzyme selectivity over SIRT1 and SIRT3. Selected compounds also exhibited generally favorable in vitro absorption, distribution, metabolism, and excretion properties. Kinetic studies revealed that a representative SIRT2 inhibitor acted competitively against both NAD⁺ and the peptide substrate, an inhibitory modality that was supported by the computational study. More importantly, two selected compounds I and II exhibited significant protection against α-synuclein aggregation-induced cytotoxicity in SH-SY5Y cells. Therefore, 5-((3-amidobenzyl)oxy)nicotinamides represent a new class of SIRT2 inhibitors that are attractive candidates for further lead optimization in the continued effort to explore selective inhibition of SIRT2 as a potential therapy for Parkinson’s disease. In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid).

4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Many triazoles have antifungal effects: the triazole antifungal drugs include fluconazole, isavuconazole, itraconazole, voriconazole, pramiconazole, ravuconazole, and posaconazole and triazole plant-protection fungicides include epoxiconazole, triadimenol, myclobutanil, propiconazole, prothioconazole, metconazole, cyproconazole, tebuconazole, flusilazole and paclobutrazol.Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid

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

Whole-cell amperometric biosensor for screening of cytochrome P450 inhibitors was written by Yoetz-Kopelman, Tal;Porat-Ophir, Carmit;Shacham-Diamand, Yosi;Freeman, Amihay. And the article was included in Sensors and Actuators, B: Chemical in 2016.Name: 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:

A fast and cost-effective whole-cell electrochem. biosensor aiming at early-stage screening of potential inhibitors of cytochrome P 450 is proposed and its feasibility demonstrated. Sensing is performed by monitoring the decrease in the electrochem. signal generated by the oxidation of the product of the enzymic reaction of cytochrome P 450 BM3 expressed in E. coli cells. The system is self-maintained and does not require enzyme purification or external addition of NADPH or other cofactors. Measurements were performed simultaneously at eight chips at low pos. potential of 100 mV vs. Ag/AgCl under continuous stirring. Kinetic anal. of aniline determination by the whole-cell system was performed and the concentration of aniline for the inhibition studies was selected accordingly. Three known inhibitors – imidazole, metyrapone and 1-aminobenzotriazole (ABT) – were tested and their inhibition profiles characterized. Imidazole was found to be the most potent inhibitor of the three. To the best of our knowledge, the system developed enables for the first time rapid and cheap cytochrome P 450 inhibitors detection by a disposable whole-cell electrochem. chip, combined with the advantages of a whole-cell system, without neither enzyme purification nor NADPH addition Furthermore, the system developed also provides capability of performing aniline detection e.g. for environmental monitoring, by means of electrochem. biosensing. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Name: 1H-Benzo[d][1,2,3]triazol-1-amine).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Name: 1H-Benzo[d][1,2,3]triazol-1-amine

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

Structural stabilization of a metal-organic framework for gas sorption investigation was written by Gao, Qiang;Zhao, Xiao-Lin;Chang, Ze;Xu, Jian;Bu, Xian-He. And the article was included in Dalton Transactions in 2016.Recommanded Product: 157069-48-2 This article mentions the following:

By inserting a ligand into a reported metal-organic framework (Co-MOF1), the reformed aggregation of triangle grids, [Co₃(μ₃-O)(cpt)₃tpt·NO₃] (Co-MOF1-tpt) (Hcpt = 4-(4′-carboxyphenyl)-1,2,4-triazole, tpt = tri(4-pyridyl)-1,3,5-triazine), shows enhanced stability. In addition, owing to its structural characteristic, the Co-MOF1-tpt also reveals a certain CO₂ storage ability and CO₂/CH₄ adsorption selectivity as expected. In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2Recommanded Product: 157069-48-2).

4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2) belongs to triazole derivatives. Triazoles are important five-member nitrogen heterocycles involved in a wide range of industrial applications such as agrochemicals, corrosion inhibitors, dyes, optical brighteners, as well as biologically active agents. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules.Recommanded Product: 157069-48-2

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

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor was written by Kung, Daniel W.;Coffey, Steven B.;Jones, Ryan M.;Cabral, Shawn;Jiao, Wenhua;Fichtner, Michael;Carpino, Philip A.;Rose, Colin R.;Hank, Richard F.;Lopaze, Michael G.;Swartz, Roger;Chen, Hou;Hendsch, Zachary;Posner, Bruce;Wielis, Christopher F.;Manning, Brian;Dubins, Jeffrey;Stock, Ingrid A.;Varma, Sam;Campbell, Mary;DeBartola, Demetria;Kosa-Maines, Rachel;Steyn, Stefanus J.;McClure, Kim F.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C9H7N3O This article mentions the following:

The discovery of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor is described. The characterization and redressing of the issues associated with these compounds is detailed. An efficient three-step synthesis and a binding assay were relied upon as the primary means of rapidly improving potency and ADMET properties for this class of inverse agonist compounds Compound 10n bearing distributed polarity in the form of an imidazo-thiazole acetamide and a Ph triazole is a unit lower in log P and has significantly improved binding affinity compared to the hit mol. 10a, providing support for further optimization of this series of compounds In the experiment, the researchers used many compounds, for example, 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3Synthetic Route of C9H7N3O).

4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3) belongs to triazole derivatives. The triazole ring is a relatively stable functional group, and the triazole bond can be used for a variety of applications, such as replacing the phosphate backbone of DNA. The presence of the three nitrogen atoms in triazole structures afforded opportunities for a plethora of structural modification with the generation of novel therapeutically potential agents, which is different from other heterocyclic compounds.Synthetic Route of C9H7N3O

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

Toxicological role of an acyl glucuronide metabolite in diclofenac-induced acute liver injury in mice was written by Oda, Shingo;Shirai, Yuji;Akai, Sho;Nakajima, Akira;Tsuneyama, Koichi;Yokoi, Tsuyoshi. And the article was included in Journal of Applied Toxicology in 2017.Reference of 1614-12-6 This article mentions the following:

The acyl glucuronide (AG) metabolites of carboxylic acid-containing drugs are potentially chem. reactive and are suggested to be implicated in toxicity, including hepatotoxicity, nephrotoxicity and drug hypersensitivity reactions. However, it remains unknown whether AG formation is related to toxicity in vivo. In this study, we sought to determine whether AG is involved in the pathogenesis of liver injury using a mouse model of diclofenac (DIC)-induced liver injury. Mice that were administered DIC alone exhibited significantly increased plasma alanine aminotransferase levels, whereas mice that were pretreated with the UDP-glucuronosyltransferase inhibitor (-)-borneol (BOR) exhibited suppressed alanine aminotransferase levels at 3 and 6 h after DIC administration although not significant at 12 h. The plasma DIC-AG concentrations were significantly lower in BOR- and DIC-treated mice than in mice treated with DIC alone. The mRNA expression levels of chemokine (C-X-C motif) ligand 1 (CXCL1), CXCL2 and the neutrophil marker CD11b were reduced in the livers of mice that had been pretreated with BOR compared to those that had been administered DIC alone, whereas mRNA expression of the macrophage marker F4/80 was not altered. An immunohistochem. anal. at 12 h samples revealed that the numbers of myeloperoxidase- and lymphocyte antigen 6 complex-pos. cells that infiltrated the liver were significantly reduced in BOR- and DIC-treated mice compared to mice that were treated with DIC alone. These results indicate that DIC-AG is partly involved in the pathogenesis of DIC-induced acute liver injury in mice by activating innate immunity and neutrophils. Copyright © 2016 John Wiley & Sons, Ltd. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Reference of 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Reference of 1614-12-6

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