Day: February 9, 2023

Zou, Ji-Yong et al. published their research in Chemical Communications (Cambridge, United Kingdom) in 2013 | CAS: 4546-95-6

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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. 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.SDS of cas: 4546-95-6

A homospin cobalt(II) topological ferrimagnet was written by Zou, Ji-Yong;Shi, Wei;Xu, Na;Li, Lei-Lei;Tang, Jin-Kui;Gao, Hong-Ling;Cui, Jian-Zhong;Cheng, Peng. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2013.SDS of cas: 4546-95-6 This article mentions the following:

An unusual 3D homospin Co(II) mol. topol. ferrimagnet was successfully assembled using a mixed ligand approach, which shows a critical temperature of 9 K and a compensation temperature of 5 K. Crystal data: orthorhombic, Fddd, a = 15.6139(8), b = 18.3439(11), c = 34.336(3) Å, Z = 16, R1 = 0.0490, wR2 = 0.1473 [I > 2σ(I)]. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6SDS of cas: 4546-95-6).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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. 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.SDS of cas: 4546-95-6

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

Chen, Di-Ming et al. published their research in Inorganic Chemistry Communications in 2019 | CAS: 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.Formula: C9H7N3O2

A polyoxometalate template metal-organic framework with unusual {Cu8(μ4-OH)6}10+ secondary building unit for photocatalytic dye degradation was written by Chen, Di-Ming;Zhang, Xue-Jing. And the article was included in Inorganic Chemistry Communications in 2019.Formula: C9H7N3O2 This article mentions the following:

The first polyoxometalate (POM)-template metal-organic framework (MOF) {(H3O)2[Cu8(μ4-OH)6Cu6(H2O)6(cpt)12](SiW12O40)3(EtOH)4(H2O)7} (1) with the {Cu8(μ4-OH)6}10+ cuboctahedron as secondary building unit has been prepared by reaction of a bifunctional organic ligand 4-(4′-carboxyphenyl)-1,2,4-triazole (Hcpt) with Cu(NO3)2·3H2O and H4SiW12O40 under hydrothermal condition. Base on the single-crystal data, complex 1 is constructed from the {Cu8(μ4-OH)6}10+ and {Cu2(CO2)4} secondary building units which are further connected by the cpt– ligands to afford the 3D framework with SiWO412– housing in the octahedral cages. Photocatalytic investigations indicate that complex 1 possesses high photocatalytic methylene blue (MB) and rhodamine B (RhB) degradation activities under visible-light irradiation In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2Formula: C9H7N3O2).

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.Formula: C9H7N3O2

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

Abramov, Aleksej et al. published their research in Phytochemistry (Elsevier) in 2021 | CAS: 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. 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.Product Details of 1614-12-6

Engineering of benzoxazinoid biosynthesis in Arabidopsis thaliana: Metabolic and physiological challenges was written by Abramov, Aleksej;Hoffmann, Thomas;Stark, Timo D.;Zheng, Linlin;Lenk, Stefan;Hammerl, Richard;Lanzl, Tobias;Dawid, Corinna;Schoen, Chris-Carolin;Schwab, Wilfried;Gierl, Alfons;Frey, Monika. And the article was included in Phytochemistry (Elsevier) in 2021.Product Details of 1614-12-6 This article mentions the following:

Plant specialised metabolites constitute a layer of chem. defense. Classes of the defense compounds are often restricted to a certain taxon of plants, e.g. benzoxazinoids (BX) are characteristically detected in grasses. BXs confer wide-range defense by controlling herbivores and microbial pathogens and are allelopathic compounds In the crops maize, wheat and rye high concentrations of BXs are synthesized at an early developmental stage. By transfer of six Bx-genes (Bx1 to Bx5 and Bx8) it was possible to establish the biosynthesis of 2,4-dihydroxy-1,4-benzoxazin-3-one glucoside (GDIBOA) in a concentration of up to 143 nmol/g dry weight in Arabidopsis thaliana. Our results indicate that inefficient channeling of substrates along the pathway and metabolisation of intermediates in host plants might be a general drawback for transgenic establishment of specialised metabolite biosynthesis pathways. As a consequence, BX levels required for defense are not obtained in Arabidopsis. We could show that indolin-2-one (ION), the first specific intermediate, is phytotoxic and is metabolised by hydroxylation and glycosylation by a wide spectrum of plants. In Arabidopsis, metabolic stress due to the enrichment of ION leads to elevated levels of salicylic acid (SA) and in addition to its intrinsic phytotoxicity, ION affects plant morphol. indirectly via SA. We could show that Bx3 has a crucial role in the evolution of the pathway, first based on its impact on flux into the pathway and, second by C3-hydroxylation of the phytotoxic ION. Thereby BX3 interferes with a supposedly generic detoxification system towards the non-specific intermediate. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Product Details 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. 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.Product Details of 1614-12-6

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

Bezencon, Olivier et al. published their research in Journal of Medicinal Chemistry in 2017 | CAS: 40594-98-7

Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeRecommanded Product: 40594-98-7

Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies was written by Bezencon, Olivier;Heidmann, Bibia;Siegrist, Romain;Stamm, Simon;Richard, Sylvia;Pozzi, Davide;Corminboeuf, Olivier;Roch, Catherine;Kessler, Melanie;Ertel, Eric A.;Reymond, Isabelle;Pfeifer, Thomas;de Kanter, Ruben;Toeroek-Schafroth, Michael;Moccia, Luca G.;Mawet, Jacques;Moon, Richard;Rey, Markus;Capeleto, Bruno;Fournier, Elvire. And the article was included in Journal of Medicinal Chemistry in 2017.Recommanded Product: 40594-98-7 This article mentions the following:

The authors report the discovery and pharmacol. characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be neg. in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478 (N-(1-((5-cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide)), which has been selected as a clin. candidate. In the experiment, the researchers used many compounds, for example, Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7Recommanded Product: 40594-98-7).

Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeRecommanded Product: 40594-98-7

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

Li, Longji et al. published their research in Angewandte Chemie, International Edition in 2020 | CAS: 1614-12-6

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) 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. 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

Catalytic Asymmetric Electrochemical α-Arylation of Cyclic β-Ketocarbonyls with Anodic Benzyne Intermediates was written by Li, Longji;Li, Yao;Fu, Niankai;Zhang, Long;Luo, Sanzhong. And the article was included in Angewandte Chemie, International Edition in 2020.Reference of 1614-12-6 This article mentions the following:

Asym. catalysis with benzyne remains elusive because of the highly fleeting and nonpolar nature of benzyne intermediates. Reported herein is an electrochem. approach for the oxidative generation of benzynes (cyclohexyne) and its successful merging with chiral primary aminocatalysis, formulating the first catalytic asym. enamine-benzyne (cyclohexyne) coupling reaction. Cobalt acetate was identified to stabilize the in situ generated arynes and facilitate its coupling with an enamine. This catalytic enamine-benzyne protocol provides a concise method for the construction of diverse α-aryl (α-cyclohexenyl) quaternary carbon stereogenic centers with good stereoselectivities. 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 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. 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

Chen, Di-Ming et al. published their research in Inorganic Chemistry in 2015 | CAS: 157069-48-2

4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2) 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. 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.Electric Literature of C9H7N3O2

Microporous Metal-Organic Framework Based on a Bifunctional Linker for Selective Sorption of CO2 over N2 and CH4 was written by Chen, Di-Ming;Zhang, Xiao-Ping;Shi, Wei;Cheng, Peng. And the article was included in Inorganic Chemistry in 2015.Electric Literature of C9H7N3O2 This article mentions the following:

A bifunctional organic linker 4-(4-carboxyphenyl)-1,2,4-triazole (HCPT), incorporating both carboxylate and triazole groups, was successfully used in the construction of a 2-fold interpenetrated dynamic metal-organic framework (MOF), {[Cu3(CPT)4(μ3-OH)]·NO3·7H2O·EtOH}n (1) based on a triangular Cu(II)-hydroxo cluster as secondary building unit (SBU). Upon solvation/desolvation and temperature, the crystal cell parameters of 1 could be fine-tuned. More importantly, a transformation from disordered phase to a more ordered phase after activation was observed via a single-crystal-to-single-crystal mode. Gas sorption studies reveal that the activated 1 exhibits highly selective sorption of CO2 over N2 and CH4 at room temperature In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2Electric Literature of C9H7N3O2).

4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2) 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. 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.Electric Literature of C9H7N3O2

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

Zhou, Xin-Hui et al. published their research in Crystallography Reports in 2017 | CAS: 4546-95-6

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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. 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.Computed Properties of C4H3N3O4

A three-dimensional coordination polymer based on 1,2,3-triazole-4,5-dicarboxylic acid (H3tda): {[Cd12(tda)8(H2O)11]·(H2O)6.25}n was written by Zhou, Xin-Hui;Chen, Qiang. And the article was included in Crystallography Reports in 2017.Computed Properties of C4H3N3O4 This article mentions the following:

The title coordination polymer {[Cd12(tda)8(H2O)11]·(H2O)6.25}n (H3tda = 1,2,3-triazole-4,5-dicarboxylic acid), has been hydrothermally synthesized and structurally characterized by single-crystal x-ray diffraction. Complex crystallizes in orthorhombic sp. gr. Pmn21 with Z = 4. The Cd2 unit doublebridged by one carboxylate oxygen atom and two neighboring nitrogen atoms from the tda3- ligands are linked by the tda3-ligands to lead to the 2D (4,4) network in the ac plane. The almost coplanar Cd2(μ5-tda)2 unit comprised of two Cd ions double-bridged by two tda3- ligands through the neighboring nitrogen atoms is connected with the other four Cd2(μ5-tda)2 units form the undulating 2D network in the ac plane. The (4,4) networks and undulating 2D networks are alternatively connected along the b axis by the tda3- ligands coordinating to the Cd ions to form the 3D framework. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6Computed Properties of C4H3N3O4).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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. 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.Computed Properties of C4H3N3O4

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

Zou, Ji-Yong et al. published their research in CrystEngComm in 2014 | CAS: 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. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Product Details of 4546-95-6

Alkaline cation directed structural diversity of cubic-cage-based cobalt(II) metal-organic frameworks: from pcu to bct net was written by Zou, Ji-Yong;Shi, Wei;Zhang, Jing-Ya;He, Yan-Fei;Gao, Hong-Ling;Cui, Jian-Zhong;Cheng, Peng. And the article was included in CrystEngComm in 2014.Product Details of 4546-95-6 This article mentions the following:

Three 2p-3d heterometallic cubic-cage-based metal-organic frameworks (MOFs), formulated as {[H2N(CH3)2]9(H3O)6[Co(H2O)6][Co8Li3(TDA)12]·14H2O}n (1), {(H3O)15[Co(H2O)6][Co8Li3(TDA)12]·10H2O}n (2) and {[H2N(CH3)2](H3O)16[Co8K5(μ2-O)(TDA)12(H2O)2]·10H2O}n (3) (H3TDA = 1H-1,2,3-triazole-4,5-dicarboxylic acid), have been successfully synthesized and structurally characterized. In these 2p-3d heterometallic cubic-cage-based MOFs, eight Co2+ cations as the vertexes are interconnected by twelve TDA3- ligands as the edges to form an unusual [Co8(TDA)12]20- cubic cage with edges of 6.12 Å, in which a hexahydrated Co2+ ion is captured for 1 and 2. The neighboring [Co8(TDA)12]20- cubic cages are further bridged by Li+ ions for 1 and 2 and K+ ions for 3 to give 3D 6-connected pcu nets for 1 and 2 and a 10-connected bct net for 3. The magnetic properties of 1–3 were studied. 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. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Product Details of 4546-95-6

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

Liu, Jiang et al. published their research in Chemical Communications (Cambridge, United Kingdom) in 2017 | CAS: 4546-95-6

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.Electric Literature of C4H3N3O4

Controllable porosity conversion of metal-organic frameworks composed of natural ingredients for drug delivery was written by Liu, Jiang;Bao, Tian-Yi;Yang, Xi-Ya;Zhu, Pei-Pei;Wu, Lian-He;Sha, Jing-Quan;Zhang, Lei;Dong, Long-Zhang;Cao, Xue-Li;Lan, Ya-Qian. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2017.Electric Literature of C4H3N3O4 This article mentions the following:

Two extremely rare β-cyclodextrin (β-CD) supported metal-organic frameworks (MOFs), CD-MOF-1 and CD-MOF-2, were induced to crystallize for the first time through a template-induced approach. The targeted CD-MOFs were employed to perform controlled drug delivery and cytotoxicity assays that confirmed their favorable biol. potential of being used as drug carriers. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6Electric Literature of C4H3N3O4).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) 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.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.Electric Literature of C4H3N3O4

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

Wang, Zhican et al. published their research in Drug Metabolism & Disposition in 2017 | CAS: 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. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeRecommanded Product: 1614-12-6

In vitro metabolism of oprozomib, an oral proteasome inhibitor: role of epoxide hydrolases and cytochrome P450s was written by Wang, Zhican;Fang, Ying;Teague, Juli;Wong, Hansen;Morisseau, Christophe;Hammock, Bruce D.;Rock, Dan A.;Wang, Zhengping. And the article was included in Drug Metabolism & Disposition in 2017.Recommanded Product: 1614-12-6 This article mentions the following:

Oprozomib is an oral proteasome inhibitor currently under investigation in patients with hematol. malignancies or solid tumors. Oprozomib elicits potent pharmacol. actions by forming a covalent bond with the active site N-terminal threonine of the 20S proteasome. Oprozomib has a short half-life across preclin. species and in patients due to systemic clearance via metabolism Potential for drug-drug interactions (DDIs) could alter the exposure of this potent therapeutic; therefore, a thorough investigation of pathways responsible for metabolism is required. In the present study, the major drug-metabolizing enzyme responsible for oprozomib metabolism was identified in vitro. A diol of oprozomib was found to be the predominant metabolite in human hepatocytes, which formed via direct epoxide hydrolysis. Using recombinant epoxide hydrolases (EHs) and selective EH inhibitors in liver microsomes, microsomal EH (mEH) but not soluble EH (sEH) was found to be responsible for oprozomib diol formation. Coincubation with 2-nonylsulfanyl-propionamide, a selective mEH inhibitor, resulted in a significant decrease in oprozomib disappearance (>80%) with concurrent complete blockage of diol formation in human hepatocytes. On the contrary, a selective sEH inhibitor did not affect oprozomib metabolism Pretreatment of hepatocytes with the pan-cytochrome P 450 (P 450) inhibitor 1-aminobenzotriazole resulted in a modest reduction (∼20%) of oprozomib metabolism These findings indicated that mEH plays a predominant role in oprozomib metabolism Further studies may be warranted to determine whether drugs that are mEH inhibitors cause clin. significant DDIs with oprozomib. On the other hand, pharmacokinetics of oprozomib is unlikely to be affected by coadministered P 450 and sEH inhibitors and/or inducers. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Recommanded Product: 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. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeRecommanded Product: 1614-12-6

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