Li, Zihuan et al. published their research in Archives of Toxicology in 2021 | CAS: 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. 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.HPLC of Formula: 1614-12-6

Potent aneugenicity of 1-methylpyrene in human cells dependent on metabolic activation by endogenous enzymes was written by Li, Zihuan;Yu, Hang;Song, Meiqi;Glatt, Hansruedi;Liu, Jianjun;Liu, Yungang. And the article was included in Archives of Toxicology in 2021.HPLC of Formula: 1614-12-6 This article mentions the following:

1-Methylpyrene (1-MP) is a common environmental pollutant and animal carcinogen. After sequential activation by cytochromes P 450 and sulfotransferases, it induced gene mutations and micronuclei in mammalian cells. In this study, 1-MP and its primary metabolite, 1-hydroxymethylpyrene (1-HMP), were investigated for the induction of centromere-pos. and neg. micronuclei in the human hepatoma cell line HepG2 and its derivatives C3A, expressing relevant enzymes at higher levels. Under a short-exposure (9 h)/long-recovery regime (2 cell cycles in total), 1-MP and 1-HMP provided neg. test results in HepG2 cells. However, they induced micronuclei in C3A cells, the effect being blocked by 1-aminobenzotriazole (inhibitor of cytochromes P450s) and reduced by pentachlorophenol (inhibitor of sulfotransferases). Immunofluorescence staining of centromere protein B in the micronuclei revealed purely clastogenic effects under this regime. Unexpectedly, 1-MP and 1-HMP at concentrations 1/5-1/4 of that required for micronuclei formation led to mitotic arrest and spindle aberrations, as detected by immunofluorescence staining of 灏? and 绾?tubulin. Thus, the chromosome-damaging mechanism of 1-MP was regime and concentration dependent: potently aneugenic under persistent exposure, while clastogenic at higher concentrations following a short-exposure/long-recovery regime. This is a convincing evidence for the existence of metabolic activation-dependent aneugens. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6HPLC of Formula: 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. 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.HPLC of Formula: 1614-12-6

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

Matsuda, Yoshiki et al. published their research in Pharmaceutical Research in 2015 | 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. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeCOA of Formula: C6H6N4

Quantitative Assessment of Intestinal First-pass Metabolism of Oral Drugs Using Portal-vein Cannulated Rats was written by Matsuda, Yoshiki;Konno, Yoshihiro;Hashimoto, Takashi;Nagai, Mika;Taguchi, Takayuki;Satsukawa, Masahiro;Yamashita, Shinji. And the article was included in Pharmaceutical Research in 2015.COA of Formula: C6H6N4 This article mentions the following:

Purpose: To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P 450 3A (CYP3A) and UDP-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs. Methods: CYP3A and UGT substrates were orally administered to portal-vein cannulated (PV) rats to evaluate their intestinal availability (Fa 璺?Fg). In the case of CYP3A substrates, vehicle or 1-aminobenzotriazole (ABT), a potent inhibitor of CYP enzymes, was pretreated to assess Fg sep. from Fa (Enzyme-inhibition method). On the other hand, since potent inhibitors of UGT have not been identified, Fg of UGT substrate was calculated from total amount of metabolites generated in enterocytes (Metabolite-distribution method). Results: After oral administration of CYP3A substrates in ABT-pretreated rats, the portal and systemic plasma concentrations of the metabolite were nearly the same, indicating almost complete inhibition of intestinal CYP3A-mediated metabolism Using Enzyme-inhibition method, Fg of midazolam (1 mg/kg) was calculated as 0.71. Addnl., total amount of raloxifene-6-glucuronide generated in enterocytes after oral administration of raloxifene was estimated using Metabolite-distribution method and Fg of raloxifene (0.98 娓璵ol/kg) was calculated as 0.21. Conclusions: PV rats enabled in vivo quant. assessment of intestinal first-pass metabolism by CYP3A and UGT. This method is useful for clarifying the cause of low bioavailability. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6COA of Formula: C6H6N4).

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. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeCOA of Formula: C6H6N4

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

Mei, Ruifeng et al. published their research in ACS Omega in 2020 | CAS: 1614-12-6

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. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Computed Properties of C6H6N4

Biotransformation of 1,8-dihydroxyanthraquinone into peniphenone under the fermentation of Aleurodiscus mirabilis was written by Mei, Ruifeng;Shi, Yaxian;Zhang, Shengqi;Hu, Juntao;Zhu, Li;Gan, Junli;Cai, Le;Ding, Zhongtao. And the article was included in ACS Omega in 2020.Computed Properties of C6H6N4 This article mentions the following:

The present study verified that 1,8-dihydroxyanthraquinone (1), a common component in some industrial raw materials and dyes, could be converted into peniphenone (2), which possesses immunosuppressive activity and other medicinal potential, by Aleurodiscus mirabilis fermentation The yield of peniphenone (2) after 7 days of fermentation was 11.05 鍗?2.19%. To reveal the transformation mechanism, two secondary metabolites, emodin (3) and monodictyphenone (4), were isolated from the fermentation broth of A. mirabilis, implying that polyketide metabolic pathways from emodin (3) to monodictyphenone (4) might exist in A. mirabilis. 1,8-Dihydroxyanthraquinone (1) was suspected to be converted into peniphenone (2) via the same pathway since emodin (3) and 1,8-dihydroxyanthraquinone (1) share very similar skeletons. The P 450 enzyme and Baeyer-Villiger oxidase in A. mirabilis were confirmed to catalyze this biotransformation on the basis of ultra-performance liquid chromatog.-mass spectrometry (UPLC-MS) anal. This novel investigation could shed light on the mechanism and therefore development of peniphenone production from 1,8-dihydroxyanthraquinone by microbial fermentation In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Computed Properties of C6H6N4).

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. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Computed Properties of C6H6N4

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

Dabak, Kadir et al. published their research in European Journal of Medicinal Chemistry in 2003 | CAS: 40594-98-7

Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7) 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 growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeCategory: triazoles

Synthesis and investigation of tuberculosis inhibition activities of some 1,2,3-triazole derivatives was written by Dabak, Kadir;Sezer, Ozkan;Akar, Ahmet;Anac, Olcay. And the article was included in European Journal of Medicinal Chemistry in 2003.Category: triazoles This article mentions the following:

In this study, 浼?diazo-灏?oxoaldehyde compounds were condensed with different amines to yield 4-acyl-1H-1,2,3-triazole derivatives The 1,2,3-triazole compounds were investigated for their inhibition activities against tuberculosis. In the experiment, the researchers used many compounds, for example, Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7Category: triazoles).

Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7) 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 growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeCategory: triazoles

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

Miyata, Atsunori et al. published their research in Xenobiotica in 2017 | CAS: 1614-12-6

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. 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.Reference of 1614-12-6

Metabolite profiling and enzyme reaction phenotyping of luseogliflozin, a sodium-glucose cotransporter 2 inhibitor, in humans was written by Miyata, Atsunori;Hasegawa, Masatoshi;Hachiuma, Kenji;Mori, Haruyuki;Horiuchi, Nobuko;Mizuno-Yasuhira, Akiko;Chino, Yukihiro;Jingu, Shigeji;Sakai, Soichi;Samukawa, Yoshishige;Nakai, Yasuhiro;Yamaguchi, Jun-ichi. And the article was included in Xenobiotica in 2017.Reference of 1614-12-6 This article mentions the following:

1. To understand the clearance mechanism of luseogliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, we investigated its human metabolite profile and metabolic enzymes responsible for the primary metabolic pathways in human using reaction phenotyping.2. Sixteen metabolites of luseogliflozin were found in human plasma and/or urine and their structural information indicated that the drug was metabolized via multiple metabolic pathways. The primary metabolic pathways involve (1) O-deethylation to form M2 and subsequent glucuronidation to form M12, (2) 锠?hydroxylation at ethoxy group to form M3 followed by oxidation to form the corresponding carboxylic acid metabolite (M17) and (3) direct glucuronidation to form M8.3. The reaction phenotyping studies indicated that the formation of M2 was mainly mediated by cytochrome P 450 (CYP) 3A4/5, and subsequently M12 formation was catalyzed by UGT1A1, UGT1A8 and UGT1A9. The formation of M3 was mediated by CYP4A11, CYP4F2 and CYP4F3B, and the further oxidation of M3 to M17 was mediated by alc. dehydrogenase and aldehyde dehydrogenase. The formation of M8 was catalyzed by UGT1A1.4. These results demonstrate that luseogliflozin is metabolized through multiple pathways, including CYP-mediated oxidation and glucuronidation, in human. 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. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. 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.Reference of 1614-12-6

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

Chen, Zhihong et al. published their research in Environmental Pollution (Oxford, United Kingdom) in 2021 | CAS: 1614-12-6

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. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Computed Properties of C6H6N4

Human CYP enzyme-activated clastogenicity of 2-ethylhexyl diphenyl phosphate (a flame retardant) in mammalian cells was written by Chen, Zhihong;Xie, Jiayi;Li, Qing;Hu, Keqi;Yang, Zongying;Yu, Hang;Liu, Yungang. And the article was included in Environmental Pollution (Oxford, United Kingdom) in 2021.Computed Properties of C6H6N4 This article mentions the following:

2-Ethylhexyl di-Ph phosphate (EHDPP) is a common flame retardant and environmental pollutant, exposing humans with endocrinal disrupting potentials. Its mutagenicity, especially following metabolism, remains unclear. In this study, mol. docking anal. indicated that EHDPP was a potential substrate for several human CYP enzymes except for CYP1A1. Among V79-derived cell lines genetically engineered for the expression of each CYP, EHDPP (6 h exposure/18 h recovery) did not induce micronuclei in the V79 or V79-derived cells expressing human CYP1A1, however, it was pos. in V79-derived cell lines expressing human CYP2E1, 3A4, and 2B6. In a human hepatoma (HepG2) cell line, EHDPP (48 h exposure) moderately induced micronuclei, which was blocked by 1-aminobenzotriazole (ABT, 60娓璏, inhibitor of CYPs); pretreating HepG2 cells with bisphenol AF, another organic pollutant as inducer of CYPs (0.1娓璏 for 16 h), significantly potentiated micronuclei formation by EHDPP, threshold being decreased from 10 to 1.25娓璏. This effect was blocked by ABT, drastically reduced by ketoconazole (inhibiting CYP3A expression/activity), and moderately inhibited by trans-1,2-dichloroethylene (selective CYP2E1 inhibitor). Immunofluorescent centromere protein B staining indicated that EHDPP-induced micronuclei in V79-derived cell lines expressing human CYP2E1 and 3A4 were predominantly centromere-neg., and that in HepG2 cells pretreated with bisphenol AF (for inducing multiple CYPs) were purely centromere-neg. In bisphenol AF-pretreated HepG2 cells EHDPP potently induced DNA breaks, as indicated by the comet assay and Western blot anal. of 绾?H2AX. In conclusion, our study suggests that EHDPP is potently clastogenic, following activation by several human CYP enzymes, CYP3A4 being a major one. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Computed Properties of C6H6N4).

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. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Computed Properties of C6H6N4

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

Matsunaga, Norikazu et al. published their research in Drug Metabolism & Disposition in 2016 | CAS: 1614-12-6

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. 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 1614-12-6

Analysis of the metabolic pathway of bosentan and of the cytotoxicity of bosentan metabolites based on a quantitative modeling of metabolism and transport in sandwich-cultured human hepatocytes was written by Matsunaga, Norikazu;Kaneko, Naomi;Yukiko, Staub Angelina;Nakanishi, Takeo;Nunoya, Ken-ichi;Imawaka, Haruo;Tamai, Ikumi. And the article was included in Drug Metabolism & Disposition in 2016.Product Details of 1614-12-6 This article mentions the following:

To quant. understand the events in the human liver, we modeled a hepatic disposition of bosentan and its three known metabolites (Ro 48-5033, Ro 47-8634, and Ro 64-1056) in sandwich cultured human hepatocytes based on the known metabolic pathway. In addition, the hepatotoxicity of Ro 47-8634 and Ro 64-1056 was investigated because bosentan is well known as a hepatotoxic drug. A model illustrating the hepatic disposition of bosentan and its three metabolites suggested the presence of a novel metabolic pathway(s) from the three metabolites. By performing in vitro metabolism studies on human liver microsomes, a novel metabolite (M4) was identified in Ro 47-8634 metabolism, and its structure was determined Moreover, by incorporating the metabolic pathway of Ro 47-8634 to M4 into the model, the hepatic disposition of bosentan and its three metabolites was successfully estimated In hepatocyte toxicity studies, the cell viability of human hepatocytes decreased after exposure to Ro 47-8634, and the observed hepatotoxicity was diminished by pretreatment with tienilic acid (CYP2C9-specific inactivator). Pretreatment with 1-aminobenzotriazole (broad cytochrome P 450 inactivator) also tended to maintain the cell viability. Furthermore, Ro 64-1056 showed hepatotoxicity in a concentration dependent manner. These results suggest that Ro 64-1056 is directly involved in bosentan-induced liver injury partly because CYP2C9 specifically mediates hydroxylation of the t-Bu group of Ro 47-8634. Our findings demonstrate the usefulness of a quant. modeling of hepatic disposition of drugs and metabolites in sandwich cultured hepatocytes. In addition, the newly identified metabolic pathway may be an alternative route that can avoid Ro 64-1056- induced liver injury. 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. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. 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 1614-12-6

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

Senthilkumar, S. et al. published their research in ACS Sustainable Chemistry & Engineering in 2018 | CAS: 157069-48-2

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. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.COA of Formula: C9H7N3O2

Pore Wall-Functionalized Luminescent Cd(II) Framework for Selective CO2 Adsorption, Highly Specific 2,4,6-Trinitrophenol Detection, and Colorimetric Sensing of Cu2+ Ions was written by Senthilkumar, S.;Goswami, Ranadip;Smith, Vincent J.;Bajaj, Hari C.;Neogi, Subhadip. And the article was included in ACS Sustainable Chemistry & Engineering in 2018.COA of Formula: C9H7N3O2 This article mentions the following:

Astute combination of basic functionality and luminescence property can pursue multifunctional metal-organic frameworks (MOFs) with assorted applications such as selective CO2 adsorption, specific detection of explosive nitro compounds, and toxic metal ion sensing. The bifunctional ligand 4-(4-carboxyphenyl)-1,2,4-triazole (HL) is used to build the framework [Cd(L)2]璺?DMF)0.92 (1) (L = L-1, DMF = N,N’-dimethylformamide), having a free N atom decorated porous channel. The solvothermal synthesis is extended to produce three isoskeletal frameworks in diverse solvents, where pore size maximizes in 2 by employing N,N’-diethylformamide solvent. The activated framework [Cd(L)2] exhibits strong CO2 affinity with good CO2/N2 selectivity, and shows min. CO2 loss during five adsorption-desorption cycles. Sensing studies for nitro-aromatic compounds in DMF reveal highly specific detection of 2,4,6-trinitophenol (TNP) with remarkable quenching (KSV = 9.3 鑴?104 M-1) and low limit of detection (LOD: 0.3 ppm). The quenching mechanism is ascribed to the combined existence of static and dynamic quenching plus resonance energy transfer. The activated framework further shows highly selective luminescent detection of Cu2+ ions with a quenching constant of 4.4 鑴?103 M-1 and very low LOD of 3.9 ppm. The detection of Cu2+ ions accompanies a visible color change in solution and solid phase, which validates the present system as a potential colorimetric Cu2+ sensor. Of note is that bifunctional sensor shows excellent reusability toward TNP and Cu2+ detection. Overall, selective and multicycle CO2 adsorption, together with efficient sensing of both TNP and Cu2+ ion, manifest this pore-functionalized MOF as a versatile material for sustainability. In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2COA of Formula: C9H7N3O2).

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. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.COA of Formula: C9H7N3O2

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

Flood, Dillon T. et al. published their research in Journal of the American Chemical Society in 2019 | CAS: 1614-12-6

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.Category: triazoles

Expanding Reactivity in DNA-Encoded Library Synthesis via Reversible Binding of DNA to an Inert Quaternary Ammonium Support was written by Flood, Dillon T.;Asai, Shota;Zhang, Xuejing;Wang, Jie;Yoon, Leonard;Adams, Zoe C.;Dillingham, Blythe C.;Sanchez, Brittany B.;Vantourout, Julien C.;Flanagan, Mark E.;Piotrowski, David W.;Richardson, Paul;Green, Samantha A.;Shenvi, Ryan A.;Chen, Jason S.;Baran, Phil S.;Dawson, Philip E.. And the article was included in Journal of the American Chemical Society in 2019.Category: triazoles This article mentions the following:

DNA Encoded Libraries have proven immensely powerful tools for lead identification. The ability to screen billions of compounds at once has spurred increasing interest in DEL development and utilization. Although DEL provides access to libraries of unprecedented size and diversity, the idiosyncratic and hydrophilic nature of the DNA tag severely limits the scope of applicable chemistries. It is known that biomacromols. can be reversibly, noncovalently adsorbed and eluted from solid supports, and this phenomenon has been utilized to perform synthetic modification of biomols. in a strategy we have described as reversible adsorption to solid support (RASS). Herein, we present the adaptation of RASS for a DEL setting, which allows reactions to be performed in organic solvents at near anhydrous conditions opening previously inaccessible chem. reactivities to DEL. The RASS approach enabled the rapid development of C(sp2)-C(sp3) decarboxylative cross-couplings with broad substrate scope, an electrochem. amination (the first electrochem. synthetic transformation performed in a DEL context), and improved reductive amination conditions. The utility of these reactions was demonstrated through a DEL-rehearsal in which all newly developed chemistries were orchestrated to afford a compound rich in diverse skeletal linkages. We believe that RASS will offer expedient access to new DEL reactivities, expanded chem. space, and ultimately more drug-like libraries. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Category: triazoles).

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.Category: triazoles

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

Xiao, Weibin et al. published their research in Xenobiotica 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.Safety of 1H-Benzo[d][1,2,3]triazol-1-amine

Inhibitory effect of ketoconazole, quinidine and 1-aminobenzotriazole on pharmacokinetics of l-tetrahydropalmatine and its metabolite in rats was written by Xiao, Weibin;Deng, Zhirong;Lai, Chongfa;Lu, Haoyang;Huang, Mutu;Wen, Yuguan;Shi, Lei. And the article was included in Xenobiotica in 2021.Safety of 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:

L-tetrahydropalmatine (l-THP) is mainly metabolised by CYP450 enzymes. This study was to investigate the possible effect of co-administered CYP inhibitors on the pharmacokinetics of l-THP and its metabolites in rats. An established LC-MS/MS method has been applied for the evaluation of drug-drug interaction between l-THP and CYP inhibitors. Following the administration of CYP inhibitors, a single dose of l-THP (9 mg/kg) was orally administrated. With regard to l-THP, the AUC0-48 were significantly increased by 4.3, 3.79, and 11.39 folds, and Cmax were increased by 4.74, 3.64, and 2.76 folds in the ketoconazole group (KET), quinidine group (QD), and 1-aminobenzotriazole group (ABT), resp. KET and QD both significantly increased the AUC0-48 of 2-DM and 2-DM-Glu by 1.38 閳?2.43 times, while Cmax was significantly decreased by 41.3 and 78.0% in the ABT group, resp. The Cmax of 3-DM was reduced by 51.38, 48.02, and 63.31% after pre-treatment with KET, QD, and ABT, resp., and Cmax of 3-DM-Glu decreased correspondingly by 29.6, 22.1, and 58.0%. Indicated that CYP inhibitors could markedly influence the systemic level of l-THP and its metabolites. To guarantee the safe use of l-THP, attention should be paid when l-THP was co-administered with CYP inhibitors, particularly with CYP3A4 and 2D6 inhibitors. 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. 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.Safety of 1H-Benzo[d][1,2,3]triazol-1-amine

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