Tag: 100-200

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

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 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

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

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

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

In 2017,Asian Journal of Chemistry included an article by Gilbile, Rohidas; Bhavani, Ram; Vyas, Ritu. Safety of Methyl 1-methyl-1H-pyrazole-4-carboxylate. The article was titled 《Evaluation of synthesis of methyl 3-chloro-5-(4,6-dimethoxypyrimidin-2-ylcarbamoylsulfamoyl)-1-methylpyrazole-4-carboxylate using green metrics》. The information in the text is summarized as follows:

A modified synthesis of Me 3-chloro-5-(4,6-dimethoxypyrimidin-2-ylcarbamoylsulfamoyl)-1-methylpyrazole-4-carboxylate (halosulfuron) was described. The merits of the synthesis were (i) one pot chlorination of Me 1-methyl-1H-pyrazole-4-carboxylate in presence of sulfuryl chloride resulting in Me 3,5-dichloro-1-methyl-1H-pyrazole-4-carboxylate (ii) conversion of 3-chloro-5-mercapto-1-methyl-1H-pyrazole-4-carboxylate to 3-chloro-1-methyl-5-sulfamoylpyrazole-4-carboxylate under mild reaction conditions utilizing tetra-Bu ammonium chloride, N-chlorosuccinimide and ammonium carbonate (iii) condensation of sulfonamide with carbamate by microwave irradiation Efforts were made to calculate, atom economy, reaction mass efficiency and E-factor for all the reaction steps involved in the synthesis of halosulfuron. The E-factor values in step 2 and step 4 reaction was lower, indicating that these reactions were greener (generation of less waste) when compared to the remaining steps in the synthesis. The experimental process involved the reaction of Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2Safety of Methyl 1-methyl-1H-pyrazole-4-carboxylate)

Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2) 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. Safety of Methyl 1-methyl-1H-pyrazole-4-carboxylate

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

Chen, Lin Zhi; Flammang, Robert; Maquestiau, Andre; Taft, Robert W.; Catalan, Javier; Cabildo, Pilar; Claramunt, Rosa M.; Elguero, Jose published an article on January 4 ,1991. The article was titled 《Thermodynamic basicity vs. kinetic basicity of diazoles (imidazoles and pyrazoles)》, and you may find the article in Journal of Organic Chemistry.Electric Literature of C7H12N2 The information in the text is summarized as follows:

The intrinsic basicity of 24 azoles (pyrazoles, indazoles, imidazoles, benzimidazoles) and 7-methylazaindole was determined by mass spectrometry techniques, ion cyclotron resonance (ICR), and/or chem. ionization (CI) in conjunction with tandem mass spectrometry (MS/MS). A reasonably good agreement (r2 = 0.967) is found between both methods (15 compounds). Thus, it is possible to use CI/MS/MS to determine the intrinsic basicity of compounds not measurable by ICR for purity or volatility reasons. Some anomalies are interpreted in terms of entropy and steric effects. The basicity data are also discussed by using empirical models (σα, σR) and chelation and annelation effects. The results came from multiple reactions, including the reaction of 1-Butyl-1H-pyrazole(cas: 52096-24-9Electric Literature of C7H12N2)

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. Electric Literature of C7H12N2

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

Application of 114474-26-9On November 30, 2013 ,《Design, synthesis, and biologic evaluation of some novel N-arylpyrazole derivatives as cytotoxic agents》 appeared in Medicinal Chemistry Research. The author of the article were Xu, Shengjie; Li, Shenghui; Tang, Yonghe; Zhang, Jinchao; Wang, Shuxiang; Zhou, Chuanqi; Li, Xiaoliu. The article conveys some information:

A novel series of N-arylpyrazole derivatives I(R = 4-CF3, 3,5-(CF3)2, 4-NO2), II, III and IV(R = H, OC8H17) has been designed and synthesized via aromatic substitution reaction of N-nonsubstituted pyrazoles with 4-fluoronitrobenzene in the presence of base. The structures of these compounds were established on the basis of elemental (C, H, and N) and spectral anal. (1H NMR, 13C NMR, HRMS, and FT-IR). All the compounds were tested for their cytotoxic activity in vitro against four human tumor cell lines: carcinoma (Bel-7402), nasopharyngeal carcinoma (KB), immature granulocyte leukemia (HL-60), and gastrocarcinoma (BGC-823) by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The results showed that most of the obtained compounds exhibited promising cytotoxicity against tested carcinoma cell lines with low IC50 values. The bis-pyrazole derivative IV(R = OC8H17), bearing alkoxy group on the 5-position of Ph ring, was the most effective one. It is inhibition of cell growth of Bel-7402 cells was 1.5-fold higher than that found for cisplatin. And, also mono-pyrazole derivatives I(R = 4-CF3, 3,5-(CF3)2) decorated with trifluoromethyl group on the Ph ring, displayed better cytotoxicity than that of cisplatin against Bel-7402 cell line. After reading the article, we found that the author used 4-(4-Nitrophenyl)-1H-pyrazole(cas: 114474-26-9Application of 114474-26-9)

4-(4-Nitrophenyl)-1H-pyrazole(cas: 114474-26-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Application of 114474-26-9

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

《Convenient synthesis of vinyldiazomethanes from α-diazo-β-keto esters and related systems》 was written by Davies, Huw M. L.; Hougland, Paul W.; Cantrell, William R. Jr.. Application of 15366-34-4This research focused onvinyldiazomethane; diazoketo ester reduction; diazohydroxy ester preparation dehydration. The article conveys some information:

A series of vinyldiazomethanes, including, RCH:CHCN2CO2R1 (R = H, R1 = Me, CMe3; R = Me, EtS, R1 = Et, Me) and CH2:CHCN2PO(OEt)2, were readily prepared by sodium borohydride reduction of α-diazo-β-keto esters, e.g., RCH2COCN2CO2R1 and MeCOCN2PO(OEt)2, followed by phosphorus oxychloride induced dehydration of the resulting α-diazo-β-hydroxy esters. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Application of 15366-34-4)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) 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.Application of 15366-34-4

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