Day: October 13, 2022

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

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

In 2016,European Journal of Organic Chemistry included an article by Belaroussi, Rabia; El Hakmaoui, Ahmed; Akssira, Mohamed; Guillaumet, Gerald; Routier, Sylvain. Electric Literature of C9H9N3O2. The article was titled 《Regioselective Synthesis of 2,4-Substituted Pyrido[1′,2′:1,5]pyrazolo[3,4-d]pyrimidines through Sequential Pd-Catalyzed Arylation and SNAr Reactions》. The information in the text is summarized as follows:

The synthesis and regioselective functionalization of rare 2,4-disubstituted-pyrido[1′,2′:1,5]pyrazolo[3,4-d]pyrimidine derivatives is reported. C-4 aminations were performed by chlorine nucleophilic substitution SNAr reactions, and their efficiencies were compared with those for direct one-pot amide C-O activation with bromotripyrrolidinophosphonium hexafluorophosphate (PyBroP) as a reagent. The latter method was used to perform palladium-catalyzed C-4 (het)arylation. Finally, two C-4 amino and aryl derivatives were prepared on a large scale and engaged in desulfurative Liebeskind-Srogl-type reactions under microwave irradiation to afford the envisioned compound library. Each step was optimized, and the results are discussed. In the experiment, the researchers used many compounds, for example, Methyl 2-aminopyrazolo[1,5-a]pyridine-3-carboxylate(cas: 1620075-73-1Electric Literature of C9H9N3O2)

Methyl 2-aminopyrazolo[1,5-a]pyridine-3-carboxylate(cas: 1620075-73-1) 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. Electric Literature of C9H9N3O2

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

Perez, Jorge D.; Yranzo, Gloria I.; Phagouape, Leonardo M. published an article on February 28 ,1986. The article was titled 《Influence of N-substitution in the FVT (flash vacuum thermolysis) of pyrazoles》, and you may find the article in Bulletin de la Societe Chimique de France.Safety of 1-Butyl-1H-pyrazole The information in the text is summarized as follows:

Flash vacuum thermolysis of 1-ethyl-, 3,5-dimethyl-1-ethyl- (I), 1-butyl-, 1-tert-butyl-, 3,5-dimethyl-1-phenyl- and 1-phenylpyrazole was studied. In the N-alkyl derivatives, pyrazole elimination and olefin formation were found. In contrast, Ph derivatives afforded isomerization and nitrogen extrusion. Kinetic parameters for compound I are described and a general mechanism including the N-H derivatives is discussed. In the part of experimental materials, we found many familiar compounds, such as 1-Butyl-1H-pyrazole(cas: 52096-24-9Safety 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. Safety of 1-Butyl-1H-pyrazole

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

In 2010,Liu, Kevin K.-C.; Bagrodia, Shubha; Bailey, Simon; Cheng, Hengmiao; Chen, Hui; Gao, Lisa; Greasley, Samantha; Hoffman, Jacqui E.; Hu, Qiyue; Johnson, Ted O.; Knighton, Dan; Liu, Zhengyu; Marx, Matthew A.; Nambu, Mitchell D.; Ninkovic, Sacha; Pascual, Bernadette; Rafidi, Kristina; Rodgers, Caroline M.-L.; Smith, Graham L.; Sun, Shaoxian; Wang, Haitao; Yang, Anle; Yuan, Jing; Zou, Aihua published 《4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Formula: C9H15BN2O2 The information in the text is summarized as follows:

Pteridinones were designed based on a non-selective kinase template. Because of the uniqueness of the PI3K and mTOR binding pockets, a Me group was introduced to C-4 position of the peteridinone core to give compounds with excellent selectivity for PI3K and mTOR. This series of compounds were further optimized to improve their potency against PI3Kα and mTOR. Finally, orally active compounds with improved solubility and robust in vivo efficacy in tumor growth inhibition were identified as well. In the part of experimental materials, we found many familiar compounds, such as 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Formula: C9H15BN2O2)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Formula: C9H15BN2O2

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

In 2014,Rossatto, Marcelo; Casanova, Caroline; Lima, Ana P.; Emmerich, Daniel J.; Oliveira, Vladimir; Dallago, Rogerio M.; Frizzo, Clarissa P.; Moreira, Dayse N.; Buriol, Lilian; Brondani, Sergio; Zanatta, Nilo; Bonacorso, Helio G.; Martins, Marcos A. P. published 《The effect of pressurized carbon dioxide on the cyclocondensation reaction between 4-alkoxy-1,1,1-trifluoro-3-alken-2-ones and hydrazines》.ARKIVOC (Gainesville, FL, United States) published the findings.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The synthesis of 1-unsubstituted and 1-phenyl-5-trifluoromethylpyrazoles from the reaction of 4-alkoxy-1,1,1-trifluoro-3-alken-2-ones [CF3C(O)CH:C(R1)OR, where R = Me, Et and R1 = H, Me, Ph] with hydrazines [NH2NHR2, where R2 = H, Ph] in pressurized carbon dioxide is reported for the first time. Reaction conditions such as pressure, temperature and time were evaluated. The methodol. developed herein was suitable to synthesize products in moderate to excellent yields (60%-96%) and short reaction times (15-45 min). In the part of experimental materials, we found many familiar compounds, such as 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole)

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.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2014,Fukuzumi, Takeo; Aikawa, Haruo; Harada, Yasue; Sugai, Ayako; Murata, Asako; Nakatani, Kazuhiko published 《Synthesis of 8-substituted adenine and adenosine libraries and the binding to pre-miR-29a》.Bulletin of the Chemical Society of Japan published the findings.Application of 844501-71-9 The information in the text is summarized as follows:

A small chem. library of 8-substituted adenine and adenosine derivatives was synthesized and examined for binding to pre-miR-29a. We found that one compound showed the affinity with 61 nM of Kd and a 10-fold stronger binding than the double-stranded RNA.3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Application of 844501-71-9) was used in this study.

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 844501-71-9

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

In 2017,Yao, Ting-Ting; Xiao, Dou-Xin; Li, Zhong-Shan; Cheng, Jing-Li; Fang, Shao-Wei; Du, Yong-Jun; Zhao, Jin-Hao; Dong, Xiao-Wu; Zhu, Guo-Nian published 《Design, Synthesis, and Fungicidal Evaluation of Novel Pyrazole-furan and Pyrazole-pyrrole Carboxamide as Succinate Dehydrogenase Inhibitors》.Journal of Agricultural and Food Chemistry published the findings.Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

The identification of novel succinate dehydrogenase (SDH) inhibitors represents one of the most attractive directions in the field of fungicide research and development. During our continuous efforts to pursue inhibitors belonging to this class, some structurally novel pyrazole-furan carboxamide and pyrazole-pyrrole carboxamide derivatives have been discovered via the introduction of scaffold hopping and bioisosterism to compound (I), a remarkably potent lead obtained by pharmacophore-based virtual screening. As a result of the evaluation against three destructive fungi, including Sclerotinia sclerotiorum, Rhizoctonia solani, and Pyricularia grisea, a majority of them displayed potent fungicidal activities. In addition to this study using 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, there are many other studies that have used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole) was used in this study.

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

HPLC of Formula: 847818-74-0In 2020 ,《Selective Halogenation of Pyridines Using Designed Phosphine Reagents》 appeared in Journal of the American Chemical Society. The author of the article were Levy, Jeffrey N.; Alegre-Requena, Juan V.; Liu, Renrong; Paton, Robert S.; McNally, Andrew. The article conveys some information:

Halopyridines are key building blocks for synthesizing pharmaceuticals, agrochems., and ligands for metal complexes, but strategies to selectively halogenate pyridine C-H precursors are lacking. We designed a set of heterocyclic phosphines that are installed at the 4-position of pyridines as phosphonium salts and then displaced with halide nucleophiles. A broad range of unactivated pyridines can be halogenated, and the method is viable for late-stage halogenation of complex pharmaceuticals. Computational studies indicate that C-halogen bond formation occurs via an SNAr pathway, and phosphine elimination is the rate-determining step. Steric interactions during C-P bond cleavage account for differences in reactivity between 2- and 3-substituted pyridines. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0HPLC of Formula: 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. HPLC of Formula: 847818-74-0

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

Category: pyrazoles-derivativesIn 2018 ,《Salicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1》 was published in Journal of Medicinal Chemistry. The article was written by Moya-Garzon, Maria Dolores; Martin Higueras, Cristina; Penalver, Pablo; Romera, Manuela; Fernandes, Miguel X.; Franco-Montalban, Francisco; Gomez-Vidal, Jose A.; Salido, Eduardo; Diaz-Gavilan, Monica. The article contains the following contents:

Primary hyperoxaluria type 1 (PH1) is a rare life-threatening genetic disease related to glyoxylate metabolism and characterized by accumulation of calcium oxalate crystals. Current therapies involve hepatic and/or renal transplantation, procedures that have significant morbidity and mortality and require long-term immunosuppression. Thus, a pharmacol. treatment is urgently needed. We introduce here an unprecedented activity of salicylic acid derivatives as agents capable of decreasing oxalate output in hyperoxaluric hepatocytes at the low micromolar range, which means a potential use in the treatment of PH1. Though correlation of this phenotypic activity with glycolate oxidase (GO) inhibition is still to be verified, most of the salicylic acids described here are GO inhibitors with IC50 values down to 3 μM. Binding mode of salicylic acids inside GO has been studied using in silico methods, and preliminary structure-activity relationships have been established. The drug-like structure and ease of synthesis of our compounds make them promising hits for structural optimization. In the experiment, the researchers used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Category: pyrazoles-derivatives)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives

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