Day: October 20, 2022

Safety of 3-(Trifluoromethyl)-1H-pyrazoleIn 2020 ,《Discovery of Pyrido[2,3-b]indole Derivatives with Gram-Negative Activity Targeting Both DNA Gyrase and Topoisomerase IV》 appeared in Journal of Medicinal Chemistry. The author of the article were Hu, Yimin; Shi, Houguang; Zhou, Mingwei; Ren, Qingcheng; Zhu, Wei; Zhang, Weixing; Zhang, Zhiwei; Zhou, Chengang; Liu, Yongqiang; Ding, Xiao; Shen, Hong C.; Yan, S. Frank; Dey, Fabian; Wu, Waikwong; Zhai, Guanglei; Zhou, Zheng; Xu, Zhiheng; Ji, Ying; Lv, Hua; Jiang, Tianyi; Wang, Wen; Xu, Yunhua; Vercruysse, Maarten; Yao, Xiangyu; Mao, Yi; Yu, Xiaomin; Bradley, Kenneth; Tan, Xuefei. The article conveys some information:

The rise of multidrug resistant (MDR) Gram-neg. (GN) pathogens and the decline of available antibiotics that can effectively treat these severe infections are a major threat to modern medicine. Developing novel antibiotics against MDR GN pathogens is particularly difficult as compounds have to permeate the GN double membrane, which has very different physicochem. properties, and have to circumvent a plethora of resistance mechanisms such as multiple efflux pumps and target modifications. The bacterial type II topoisomerases DNA gyrase (GyrA2B2) and Topoisomerase IV (ParC2E2) are highly conserved targets across all bacterial species and validated in the clinic by the fluoroquinolones. Dual inhibitors targeting the ATPase domains (GyrB/ParE) of type II topoisomerases can overcome target-based fluoroquinolone resistance. However, few ATPase inhibitors are active against GN pathogens. In this study, we demonstrated a successful strategy to convert a 2-carboxamide substituted azaindole chem. scaffold with only Gram-pos. (GP) activity into a novel series with also potent activity against a range of MDR GN pathogens. By systematically fine-tuning the many physicochem. properties, we identified lead compounds such as 17r with a balanced profile showing potent GN activity, high aqueous solubility, and desirable PK features. Moreover, we showed the bactericidal efficacy of 17r using a neutropenic mouse thigh infection model.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Safety of 3-(Trifluoromethyl)-1H-pyrazole) was used in this study.

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) 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.Safety of 3-(Trifluoromethyl)-1H-pyrazole

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

Application In Synthesis of 1-Butyl-1H-pyrazoleOn November 30, 2014 ,《Proton Transfer Reaction Time-of-Flight Mass Spectrometric (PTR-TOF-MS) determination of volatile organic compounds (VOCs) emitted from a biomass fire developed under stable nocturnal conditions》 appeared in Atmospheric Environment. The author of the article were Brilli, Federico; Gioli, Beniamino; Ciccioli, Paolo; Zona, Donatella; Loreto, Francesco; Janssens, Ivan A.; Ceulemans, Reinhart. The article conveys some information:

Combustion of solid and liquid fuels is the largest source of potentially toxic volatile organic compounds (VOCs), which can strongly affect health and the phys. and chem. properties of the atm. Among combustion processes, biomass burning is one of the largest at global scale. We used a Proton Transfer Reaction “”Time-of-Flight”” Mass Spectrometer (PTR-TOF-MS), which couples high sensitivity with high mass resolution, for real-time detection of multiple VOCs emitted by burned hay and straw in a barn located near our measuring station. We detected 132 different organic ions directly attributable to VOCs emitted from the fire. Methanol, acetaldehyde, acetone, Me vinyl ether (MVE), acetic acid and glycolaldehyde dominated the VOC mixture composition The time-course of the 25 most abundant VOCs, representing ∼85% of the whole mixture of VOCs, was associated with that of carbon monoxide (CO), carbon dioxide (CO2) and methane (CH4) emissions. The strong linear relationship between the concentrations of pyrogenic VOC and of a reference species (i.e. CO) allowed us to compile a list of emission ratios (ERs) and emission factors (EFs), but values of ER (and EF) were overestimated due to the limited mixing of the gases under the stable (non-turbulent) nocturnal conditions. In addition to the 25 most abundant VOCs, chem. formula and concentrations of the residual, less abundant VOCs in the emitted mixture were also estimated by PTR-TOF-MS. Furthermore, the evolution of the complex combustion process was described on the basis of the diverse types of pyrogenic gases recorded. The experimental part of the paper was very detailed, including the reaction process of 1-Butyl-1H-pyrazole(cas: 52096-24-9Application In Synthesis of 1-Butyl-1H-pyrazole)

1-Butyl-1H-pyrazole(cas: 52096-24-9) 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 In Synthesis of 1-Butyl-1H-pyrazole

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

Recommanded Product: 930-36-9On November 1, 2019 ,《Hydroxyl-functionalized pyrazolium ionic liquids to catalyze chemical fixation of CO2: Further benign reaction condition for the single-component catalyst》 appeared in Journal of Molecular Liquids. The author of the article were Wang, Tengfei; Ma, Yuan; Jiang, Jiamin; Zhu, Xinrui; Fan, Baowan; Yu, Guanyao; Li, Ningning; Wang, Shasha; Ren, Tiegang; Wang, Li; Zhang, Jinglai. The article conveys some information:

Lots of ionic liquids have been utilized as catalyst for the coupling reaction of carbon dioxide with epoxides; however, catalyzed conditions could not be regarded as benign, especially when no co-catalyst and/or organic solvent is involved. A series of hydroxyl-functionalized pyrazolium ionic liquids are firstly synthesized. They would efficiently catalyze the cycloaddition of carbon dioxide and propylene oxide under 110°C and 1.0 MPa carbon dioxide initial pressure with 1 mol% catalyst during 4 h resulting in the product yield of 91.2%. The catalytic condition is greatly refined as compared with other single-component ionic liquids with simple anion. Simultaneously, the effect of reaction temperature, amount of catalyst, carbon dioxide initial pressure, and reaction time is explored along with the reusability of catalyst. For most of epoxides with terminal substituted group, HEEPzBr presents acceptable catalytic activity. The difference of HEMPzBr, HEEPzBr, and HPEPzBr is also explored by the d. functional theory calculations The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Recommanded Product: 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. Recommanded Product: 930-36-9

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

Application In Synthesis of 1-MethylpyrazoleOn June 9, 2022, Rong, Deqin; Zhou, Kaixin; Fang, Wei; Yang, Hong; Zhang, Yi; Shi, Qiongyu; Huang, Yuting; Li, Jiayi; Dong, Hui; Li, Lanlan; Ding, Jian; Huang, Xun; Wang, Yuanxiang published an article in Journal of Medicinal Chemistry. The article was 《Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5》. The article mentions the following:

PRMT5 is a major type II protein arginine methyltransferase and plays important roles in diverse cellular processes. Overexpression of PRMT5 is implicated in various types of cancer. Many efforts have been made to develop potent and selective PRMT5 inhibitors, the most potent of which is usually derived from nucleoside structures. Here, we designed a novel series of non-nucleoside PRMT5 inhibitors through the structure-aided drug design approach. SAR exploration and metabolic stability optimization led to the discovery of compound 41 as a potent PRMT5 inhibitor with good selectivity. Addnl., compound 41 exerted antiproliferative effects against A375 cells by inducing apoptosis and potently inhibited the methyltransferase activity of PRMT5 in cells. Moreover, it showed attractive pharmacokinetic properties and markedly suppressed the tumor growth in an A375 tumor xenograft model. These results clearly indicate that 41 is a highly potent and selective non-nucleoside PRMT5 inhibitor. The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9Application In Synthesis 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. Application In Synthesis of 1-Methylpyrazole

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

Quality Control of 1-MethylpyrazoleOn March 25, 2021, Shi, Xinzhe; Sosa Carrizo, E. Daiann; Cordier, Marie; Roger, Julien; Pirio, Nadine; Hierso, Jean-Cyrille; Fleurat-Lessard, Paul; Soule, Jean-Francois; Doucet, Henri published an article in Chemistry – A European Journal. The article was 《C-H Bond Arylation of Pyrazoles at the β-Position: General Conditions and Computational Elucidation for a High Regioselectivity》. The article mentions the following:

Direct arylation of most five-membered ring heterocycles are generally easily accessible and strongly favored at the α-position using classical palladium-catalysis. Conversely, regioselective functionalization of such heterocycles at the concurrent β-position remains currently very challenging. Herein, authors report general conditions for regioselective direct arylation at the β-position of pyrazoles, while C-H α-position is free. By using aryl bromides as the aryl source and a judicious choice of solvent, the arylation reaction of variously N-substituted pyrazoles simply proceeds via β-C-H bond functionalization. The β-regioselectivity is promoted by a ligand-free palladium catalyst and a simple base without oxidant or further additive, and tolerates a variety of substituents on the bromoarene. DFT calculations revealed that a protic solvent such as 2-ethoxyethan-1-ol significantly enhances the acidity of the proton at β-position of the pyrazoles and thus favors this direct β-C-H bond arylation. This selective pyrazoles β-C-H bond arylation was successfully applied for the straightforward building of π-extended poly(hetero)aromatic structures via further Pd-catalyzed combined α-C-H intermol. and intramol. C-H bond arylation in an overall highly atom-economical process. The results came from multiple reactions, including the reaction of 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

HPLC of Formula: 930-36-9On June 7, 2019, Iida, Keisuke; Ishida, Shunsuke; Watanabe, Takamichi; Arai, Takayoshi published an article in Journal of Organic Chemistry. The article was 《Disulfide-Catalyzed Iodination of Electron-Rich Aromatic Compounds》. The article mentions the following:

Herein, a disulfide-catalyzed electrophilic iodination of aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) has been developed. The disulfide activates DIH as a Lewis base to promote the iodination reaction in acetonitrile under mild conditions. This system is applicable to a wide range of electron-rich aromatic compounds, including acetanilide, anisole, imidazole, and pyrazole derivatives In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9HPLC of Formula: 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. HPLC of Formula: 930-36-9

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

Pu, Jun; Kreft, Anthony F.; Aschmies, Suzan H.; Atchison, Kevin P.; Berkowitz, Joshua; Caggiano, Thomas J.; Chlenov, Micheal; Diamantidis, George; Harrison, Boyd L.; Hu, Yun; Huryn, Donna; Steven Jacobsen, J.; Jin, Mei; Lipinski, Kerri; Lu, Peimin; Martone, Robert L.; Morris, Koi; Sonnenberg-Reines, June; Riddell, Dave R.; Sabalski, Joan; Sun, Shaiu-Ching; Wagner, Erik; Wang, Yiqun; Xu, Zheng; Zhou, Hua; Resnick, Lynn published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors》.Recommanded Product: 52096-24-9 The author mentioned the following in the article:

γ-Secretase inhibitors have been shown to reduce the production of β-amyloid, a component of the plaques that are found in brains of patients with Alzheimer’s disease. A novel series of heterocyclic sulfonamide γ-secretase inhibitors that reduce β-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative γ-secretase substrate. The results came from multiple reactions, including the reaction of 1-Butyl-1H-pyrazole(cas: 52096-24-9Recommanded Product: 52096-24-9)

1-Butyl-1H-pyrazole(cas: 52096-24-9) 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. Recommanded Product: 52096-24-9

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

In 1999,Storer, Richard; Ashton, Claire J.; Baxter, Anthony D.; Hann, Michael M.; Marr, Clara L. P.; Mason, Andrew M.; Mo, Chi-Leung; Myers, Peter L.; Noble, Stewart A.; Penn, Harles R.; Weir, Niall G.; Woods, Jacqueline M.; Coe, Paul L. published 《The synthesis and antiviral activity of 4-fluoro-1-β-D-ribofuranosyl-1H-pyrazole-3-carboxamide》.Nucleosides & Nucleotides published the findings.COA of Formula: C5H6N2O2 The information in the text is summarized as follows:

A novel fluoropyrazole ribonucleoside has been shown to have significant anti-influenza activity in vitro. The compound is compared and contrasted with the structurally-related compound ribavirin in attempts to identify factors having significant bearing on the mode of action of both compounds The experimental process involved the reaction of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4COA of Formula: C5H6N2O2)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.COA of Formula: C5H6N2O2

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

In 2011,Deng, Xiaohu; Roessler, Armin; Brdar, Ivana; Faessler, Roger; Wu, Jiejun; Sales, Zachary S.; Mani, Neelakandha S. published 《Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3》.Journal of Organic Chemistry published the findings.Related Products of 20154-03-4 The information in the text is summarized as follows:

A POCl3-mediated, direct amination reaction of heterocyclic amides/ureas with NH-heterocycles or N-substituted anilines is described. Compared to the existing methods, this operationally simple protocol provides unique reactivity and functional group compatibility because of the metal-free, acidic reaction conditions. The yields are generally excellent. The results came from multiple reactions, including the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Related Products of 20154-03-4)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Related Products of 20154-03-4

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

In 2017,Lee, Eun; An, Ying; Kwon, Junhee; Kim, Keun Il; Jeon, Raok published 《Optimization and biological evaluation of 2-aminobenzothiazole derivatives as Aurora B kinase inhibitors》.Bioorganic & Medicinal Chemistry published the findings.Product Details of 15366-34-4 The information in the text is summarized as follows:

A strong relationship between abnormal functions of Aurora kinases and tumorigenesis has been reported for decades. Consequently, Aurora kinases serve as potential targets for anticancer agents. Here, we identified aminobenzothiazole derivatives as novel inhibitors of Aurora B kinase through bioisosteric replacement of the previous inhibitors, aminobenzoxazole derivatives Most of the urea-linked aminobenzothiazole derivatives showed potent and selective inhibitory activity against Aurora B kinase over Aurora A kinase. Mol. modeling indicated that compound I bound well to the active site of Aurora B kinase and formed the essential hydrogen bonds. The potent compounds, I and II, were selected, and their biol. effects were evaluated using HeLa cell lines. It was found that these compounds inhibited the phosphorylation of histone H3 at Ser10 and induced G2/M cell cycle arrest. We suggest that the reported compounds have the potential to be further developed as anticancer therapeutics. In addition to this study using Methyl 1H-pyrazole-3-carboxylate, there are many other studies that have used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Product Details of 15366-34-4) was used in this study.

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Product Details of 15366-34-4

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