Category: 930-36-9

《Cytochrome P450 1A2 is the most important enzyme for hepatic metabolism of the metamizole metabolite 4-methylaminoantipyrine》 was written by Bachmann, Fabio; Meyer zu Schwabedissen, Henriette E.; Duthaler, Urs; Krahenbuehl, Stephan. Electric Literature of C4H6N2 And the article was included in British Journal of Clinical Pharmacology on April 30 ,2022. The article conveys some information:

Metamizole (dipyrone) is a prodrug not detectable in serum or urine after oral ingestion. The primary metabolite, 4-methylaminoantipyrine (4-MAA), can be N-demethylated to 4-aminoantipyrine (4-AA) or oxidized to 4-formylaminoantipyrine (4-FAA) by cytochrome P 450 (CYP)-dependent reactions. We aimed to identify the CYPs involved in 4-MAA metabolism and to quantify the effect of CYP inhibition on 4-MAA metabolism We investigated the metabolism of 4-MAA in vitro using CYP expressing supersomes and the pharmacokinetics of metamizole in the presence of CYP inhibitors in male subjects. The experiments in supersomes revealed CYP1A2 as the major CYP for 4-MAA N-demethylation and 4-FAA formation with CYP2C19 and CYP2D6 contributing to N-demethylation. In the clin. study, we investigated the influence of ciprofloxacin (CYP1A2 inhibitor), fluconazole (CYP2C19 inhibitor) and the combination ciprofloxacin/fluconazole on the pharmacokinetics of metamizole in n = 12 male subjects in a randomized, placebo-controlled, double-blind study. The geometric mean ratios for the area under the concentration-time curve of 4-MAA after/before treatment were 1.17 (90% CI 1.09-1.25) for fluconazole, 1.51 (90% CI 1.42-1.60) for ciprofloxacin and 1.92 (90% CI 1.81-2.03) for ciprofloxacin/fluconazole. Fluconazole increased the half-life of 4-MAA from 3.22 h by 0.47 h (95% CI 0.13-0.81, P < .05), ciprofloxacin by 0.69 h (95% CI 0.44-0.94, P < .001) and fluconazole/ciprofloxacin by 2.85 h (95% CI 2.48-3.22, P < .001). CYP1A2 is the major CYP for the conversion of 4-MAA to 4-AA and 4-FAA. The increase in 4-MAA exposure by the inhibition of CYP1A2 and by the combination CYP1A2/CYP2C19 may be relevant for dose-dependent adverse reactions of 4-MAA. In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Electric Literature of C4H6N2) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Electric Literature of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Abu Talip, Ruwaida Asyikin; Yahya, Wan Zaireen Nisa; Bustam, Mohamad Azmi published an article on January 15 ,2022. The article was titled 《Understanding the physicochemical and transport properties of pyrazolium based ionic liquids bearing iodide and triiodide anions》, and you may find the article in Journal of Molecular Liquids.Reference of 1-Methylpyrazole The information in the text is summarized as follows:

Ionic liquids (ILs) particularly imidazolium-based ILs have been widely used in various industrial applications such as solvent or catalyst for synthesis, as electrolyte in energy devices, and as solvent for extraction and separation The extensive phys. and chem. properties data available on the imidazolium-based ILs have made them easier to be incorporated into variety of applications compared to other types of ionic liquids Ionic liquids composed of pyrazolium derivative as cation having the same heteroaromatic ring structure with imidazolium derivative except for the position of the nitrogen atoms, may result in unique phys. and chem. properties, yet have been minimally explored. The main objective of this study is to investigate the physicochem. and transport properties of pyrazolium-based ILs to fully comprehend their potential for further development for a specific task or application. In this study, three alkylpyrazolium iodides ILs as well as corresponding three alkylpyrazolium triiodides ILs were synthesized and characterized. The NMR anal. showed that the formation of alkylpyrazolium triiodides ILs from their resp. iodide precursors has resulted the resonance to be more deshielded due to lesser electron d. experienced by the acidic protons of pyrazolium cation due to the weakly localized charge in triiodide anion. The effect of different anions and the alkyl chain of the pyrazolium cation moiety has a pronounced effect on the phys. and transport properties of the synthesized ILs. It is found that the pyrazolium ionic liquids with triiodide anion demonstrated high thermal stability, low viscosity, and high ionic conductivity as compared to the iodide analogs.1-Methylpyrazole(cas: 930-36-9Reference of 1-Methylpyrazole) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Reference of 1-Methylpyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Computed Properties of C4H6N2On May 20, 2022 ,《Continuous Processing of Concentrated Organolithiums in Flow Using Static and Dynamic Spinning Disc Reactor Technologies》 appeared in Organic Process Research & Development. The author of the article were Wietelmann, Ulrich; Kloesener, Johannes; Rittmeyer, Peter; Schnippering, Stefan; Bats, Henk; Stam, Wouter. The article conveys some information:

Organometallic reactions involving highly reactive organolithium reagents are widely used in organic synthesis. However, the use of organometallics in batch mode on a pilot and industrial scale is challenging for safety reasons and frequently requires expensive cryogenic process conditions. A change to continuous processing in flow mode can provide major advantages for process safety and economics. In this study, we compare static and dynamic flow reactor technologies for two important organolithium (butyllithium and hexyllithium)-enabled transformations: deprotonations and bromine/lithium exchange reactions. Using higher concentrated (≥3 M) butyllithium (BuLi) solutions, i.e., reaction mixtures with reduced hydrocarbon content, decreases the risk of reactor fouling and allows for increased space/time yields. In the flow mode, the observed reactions could be carried out under more convenient conditions, i.e., at higher temperatures compared to the batch mode, and the deprotonation reaction even at ambient temperature instead of -78°C. The formation of precipitates with the risk of clogging can be further reduced by changing from static flow to dynamic spinning disk reactor technol. The SpinPro reactor system from Flowid has been identified to ensure robust performance, as it tolerates salt precipitations and can provide excellent mass transfer conditions. Flow process technol. using concentrated organolithium products can provide unique benefits for the manufacturing of pharmaceutical intermediates, agrochem. products, and specialty chems. After reading the article, we found that the author used 1-Methylpyrazole(cas: 930-36-9Computed Properties of C4H6N2)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Computed Properties of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Application of 930-36-9On November 1, 2021 ,《Design, synthesis and biological evaluation of naphthalene-derived (arylalkyl)azoles containing heterocyclic linkers as new anticonvulsants: A comprehensive in silico, in vitro, and in vivo study》 appeared in European Journal of Pharmaceutical Sciences. The author of the article were Valipour, Mehdi; Naderi, Nima; Heidarli, Elmira; Shaki, Fatemeh; Motafeghi, Farzaneh; Talebpour Amiri, Fereshteh; Emami, Saeed; Irannejad, Hamid. The article conveys some information:

In continuation of our research to find strong and safe anticonvulsant agents, a number of (arylalkyl)azoles (AAAs) containing naphthylthiazole and naphthyloxazole scaffolds were designed and synthesized. The in vivo anticonvulsant evaluations in BALB/c mice revealed that some of them had significant anticonvulsant activity in both maximal electroshock (MES) and pentylenetetrazole (PTZ) models of epilepsy. The best profile of activity was observed with compounds containing imidazole and triazole rings (C1, C6, G1, and G6). In particular, imidazolylmethyl-thiazole C1 with median ED (ED50)= 7.9 mg/kg in the MES test, ED50= 27.9 mg/kg in PTZ test, and without any sign of neurotoxicity (in the rotarod test, 100 mg/kg) was the most promising compound The patch-clamp recording was performed to study the mechanism of action of the representative compound C1 on hippocampal dentate gyrus (DG) cells. The results did not confirm any modulatory effect of C1 on the voltage-gated ion channels (VGICs) or GABAA agonism, but suggested a significant reduction of excitatory postsynaptic currents (EPSCs) frequency on hippocampal DG neurons. Sub-acute toxicity studies revealed that administration of the most active compounds (C1, C6, G1, and G6) at 100 mg/kg bw/day for two weeks did not result in any mortality or significant toxicity as evaluated by assessment of biochem. markers such as lipid peroxidation, intracellular glutathione, total antioxidant capacity, histopathol. changes, and mitochondrial functions. Other pharmacol. aspects of compounds including mechanistic and ADME properties were investigated computationally and/or exptl. Mol. docking on the NMDA and AMPA targets suggested that the introduction of the heterocyclic ring in the middle of AAAs significantly affects the affinity of the compounds The obtained results totally demonstrated that the prototype compound C1 can be considered as a new lead for the development of anticonvulsant agents. In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Application of 930-36-9) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Application of 930-36-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Synthetic Route of C4H6N2On June 7, 2021, Alvarez, Eva Maria; Karl, Teresa; Berger, Florian; Torkowski, Luca; Ritter, Tobias published an article in Angewandte Chemie, International Edition. The article was 《Late-Stage Heteroarylation of Hetero(aryl)sulfonium Salts Activated by α-Amino Alkyl Radicals》. The article mentions the following:

We report a late-stage heteroarylation of aryl sulfonium salts through activation with α-amino alkyl radicals in a mechanistically distinct approach from previously reported halogen-atom transfer (XAT). The new mode of activation of aryl sulfonium salts proceeds in the absence of light and photoredox catalysts, engaging a wide range of heteroarenes. Furthermore, we demonstrate the applicability of this methodol. in synthetically useful cross-coupling transformations. In the experiment, the researchers used many compounds, for example, 1-Methylpyrazole(cas: 930-36-9Synthetic Route of C4H6N2)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Synthetic Route of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2021,Chemical Communications (Cambridge, United Kingdom) included an article by Hara, Naofumi; Uemura, Nao; Nakao, Yoshiaki. Quality Control of 1-Methylpyrazole. The article was titled 《C2-Selective silylation of pyridines by a rhodium-aluminum complex》. The information in the text is summarized as follows:

We have developed a C2-selective dehydrogenative mono-silylation of a variety of pyridines using a Rh-Al complex [(R2PCH2N-1,2-C6H4NMe-1,2-C6H4NCH2PR2)AlClRhCl(L)]n (R = Ph, iPr; n = 1, L = nbd; n = 2, L void). Both the site- and mono-selectivity are controlled via the pyridine coordination to the Lewis-acidic Al center prior to the activation of the pyridine C(2)-H bond at the proximal Rh center. A reaction mechanism is proposed based on several mechanistic studies, including the isolation of a (2-pyridyl)silylrhodium intermediate. In the experimental materials used by the author, we found 1-Methylpyrazole(cas: 930-36-9Quality Control of 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Quality Control of 1-Methylpyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Toxicity of azoles towards the anaerobic ammonium oxidation (anammox) process》 was written by Lakhey, Nivrutti; Li, Guangbin; Sierra-Alvarez, Reyes; Field, Jim A.. Computed Properties of C4H6N2 And the article was included in Journal of Chemical Technology and Biotechnology on April 30 ,2020. The article conveys some information:

Azoles are an important class of compounds that are widely used as corrosion inhibitors in aircraft de-icing agents, cooling towers, semiconductor manufacturing and household dishwashing detergents. They also are important moieties in pharmaceutical drugs and fungicides. Azoles are widespread emerging contaminants occurring frequently in water bodies. Azole compounds can potentially cause inhibition towards key biol. processes in natural ecosystems and wastewater treatment processes. Of particular concern is the inhibition of azoles to the nitrification process (aerobic oxidation of ammonium). This study investigated the acute toxicity of azole compounds towards the anaerobic ammonia oxidation (anammox) process, which is an important environmental biotechnol. gaining traction for nutrient-nitrogen removal during wastewater treatment. In this study, using batch bioassay techniques, the anammox toxicity of eight commonly occurring azole compounds was evaluated. The results show that 1H-benzotriazole and 5-methyl-1H-benzotriazole had the highest inhibitory effect on the anammox process, causing 50% decrease in anammox activity (IC50) at concentrations of 19.6 and 17.8 mg L-1, resp. 1H-imidazole caused less severe toxicity with an IC50 of 79.4 mg L-1. The other azole compounds were either nontoxic (1H-pyrazole, 1H-1,2,4-triazole and 1-methyl-pyrazole) or at best mildly toxic (1H-benzotriazole-5-carboxylic acid and 3,5-dimethyl-1H-pyrazole) towards the anammox bacteria at the concentrations tested. This study showed that most azole compounds tested displayed mild to low or no toxicity towards the anammox bacteria. The anammox bacteria were found to be far less sensitive to azoles compared to nitrifying bacteria.1-Methylpyrazole(cas: 930-36-9Computed Properties of C4H6N2) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Computed Properties of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

The author of 《Prediction of 15N NMR chemical shifts for nitrogenated aromatic compounds》 were de Oliveira, Marcelo T.; Alves, Julia M. A.; de A. Morais, Sara F.; Braga, Ataualpa A. C.. And the article was published in ARKIVOC (Gainesville, FL, United States) in 2020. SDS of cas: 930-36-9 The author mentioned the following in the article:

Building on recent developments, we compare performance of two distinct protocols, namely SMD-mPW1PW91/6-311+G(2d,p) and CPCM-OLYP/pcSseg-2, for the computation of 15N chem. shifts of nitrogenated aromatic compounds The latter shows best overall performance (MAD 5.3 ppm) albeit results in chloroform favors the former. The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9SDS of cas: 930-36-9)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. SDS of cas: 930-36-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Product Details of 930-36-9On May 31, 2022, Zhakupbekova, Aray; Baimatova, Nassiba; Psillakis, Elefteria; Kenessov, Bulat published an article in Environmental Science and Pollution Research. The article was 《Quantification of trace transformation products of rocket fuel unsymmetrical dimethylhydrazine in sand using vacuum-assisted headspace solid-phase microextraction》. The article mentions the following:

Quantification of unsym. dimethylhydrazine transformation products in solid samples is an important stage in monitoring of environmental pollution caused by heavy rockets launches. The new method for simultaneous quantification of unsym. dimethylhydrazine transformation products in sand samples using vacuum-assisted headspace solid-phase microextraction without addition of water followed by gas chromatog.-mass spectrometry is proposed. Decreasing air evacuation time from 120 to 20 s at 23°C resulted in increased responses of analytes by 25-46% and allowed obtaining similar responses as after evacuation at -30°C. The best combination of responses of analytes and their relative standard deviations (RSDs) was achieved after air evacuation of a sample (m = 1.00 g) for 20 s at 23°C, incubation for 30 min at 40°C, and 30-min extraction at 40°C by Carboxen/polydimethylsiloxane (Car/PDMS) fiber. The method was validated in terms of linearity (R2=0.9912-0.9938), limits of detection (0.035 to 3.6 ng g-1), limits of quantification (0.12-12 ng g-1), recovery (84-97% with RSDs 1-11%), repeatability (RSDs 3-9%), and reproducibility (RSDs 7-11%). It has a number of major advantages over existing methods based on headspace solid-phase microextraction-lower detection limits, better accuracy and precision at similar or lower cost of sample preparation The developed method was successfully applied for studying losses of analytes from open vials with model sand spiked with unsym. dimethylhydrazine transformation products. It can be recommended for anal. of trace concentrations of unsym. dimethylhydrazine transformation products when studying their transformation, migration and distribution in contaminated sand. After reading the article, we found that the author used 1-Methylpyrazole(cas: 930-36-9Product Details of 930-36-9)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Product Details of 930-36-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

The author of 《Analysis of bio-active compounds present in the leaves and stem of Trichosanthes roxb. using GC-MS technique with respect to its anti-inflammatory action》 were Aravindakshan, Aghil Soorya; Thangavel, Sekar. And the article was published in International Journal of Pharmacy and Pharmaceutical Sciences in 2021. Synthetic Route of C4H6N2 The author mentioned the following in the article:

Structural elucidation studies on Trichosanthes lobata Et acetate and methanol extracts of leaf and stem parts through Gas Chromatog.-Mass Spectrometry (GC-MS) technique with respect to anti-inflammatory potential. Extracts obtained with shade dried and powd. samples in successive solvent extraction using Et acetate and methanol by Soxhlet apparatus and subjected to GC-MS anal. and interpreted for its anti-inflammatory compounds The study revealed that the extraction solvent used was able to recover compound of classes such as organic acid esters and conjugated alkaloids in larger quantities than other classes of compounds and they varied with leaf and stem and also with the polarity of solvents used. In total compounds identified, GC-MS profile of the Et Acetate leaf extract of T. lobata contained 41 compounds, stem extract contained 45 compounds which have reported bioassays in PubChem. Whereas GC-MS profile of methanol leaf extract of T. lobata contained 66 compounds and stem extract contained 46 compounds having bioassay reports in PubChem. A large number of phytochem. peaks with good area percentage were found in methanolic extract We were also able to find out potent anti-inflammatory compounds including Octanoic acid, Dodecanoic acid, Octadecane, Enoic acid, Hexanoic acid, Quinazolin-8-one, Ilicic acid, Pentadecanoic acid, Oxaspiro, Benzeneacetic acid, etc. from the extracts T. lobata contains phytocompounds against inflammation which may serve as a new drug lead of natural products origin in future and make it employable in modern pharmacol. practices.1-Methylpyrazole(cas: 930-36-9Synthetic Route of C4H6N2) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Synthetic Route of C4H6N2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics