pyrazoles-derivatives

In 2016,Diamanti, Eleonora; Bottegoni, Giovanni; Goldoni, Luca; Realini, Natalia; Pagliuca, Chiara; Bertozzi, Fabio; Piomelli, Daniele; Pizzirani, Daniela published 《Pyrazole-Based Acid Ceramidase Inhibitors: Design, Synthesis, and Structure-Activity Relationships》.Synthesis published the findings.Related Products of 20154-03-4 The information in the text is summarized as follows:

Acid ceramidase (a.c.) is a lysosomal cysteine amidase responsible for the cleavage of ceramide into sphingosine, which is then phosphorylated to sphingosine 1-phosphate. AC regulates the intracellular levels of ceramide and sphingosine, and a.c. inhibition may be useful in the treatment of disorders, such as cancer, in which ceramide-mediated signaling may be dysfunctional. Despite their potential exptl. and therapeutic value, the number of available small-mol. inhibitors of a.c. activity remains limited. In the present study is described the discovery of a class of potent pyrazole carboxamide-based a.c. inhibitors, which were identified using the at. property field (APF) approach and developed through systematic SAR studies and in vitro pharmacol. characterization. The best compound of this series inhibits a.c. with nanomolar potency and causes ceramide accumulation and sphingosine depletion in intact G361 proliferative melanoma cells. By expanding the current armamentarium of a.c. inhibitors, these results should facilitate future efforts to unravel the biol. of a.c. and the therapeutic potential of its inhibition.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Related Products of 20154-03-4) was used in this study.

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,Diaz, Jose Luis; Corbera, Jordi; Martinez, Daniel; Bordas, Magda; Sicre, Cristina; Pascual, Rosalia; Pretel, Ma Jose; Marin, Ana Paz; Montero, Ana; Dordal, Albert; Alvarez, Ines; Almansa, Carmen published 《Pyrazolo[3,4-d]pyrimidines as sigma-1 receptor ligands for the treatment of pain. Part 2: Introduction of cyclic substituents in position 4》.MedChemComm published the findings.Name: 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 replacement of acylamino group by cyclic substituents in the position 4 of the pyrazolo[3,4-d]pyrimidine scaffold I [R = Ph, pyridin-3-yl, 1-methyl-1H-pyrazol-5-yl, etc.], led to highly active sigma-1 receptor (σ1R) ligands. Ph or pyrazolyl groups were the best in terms of affinity for the σ1R and the compound I [R = 1-methyl-1H-pyrazol-5-yl], was the most selective. Compound I [R = 1-methyl-1H-pyrazol-5-yl] was also one of the best σ1R ligands ever described in terms of lipophilic ligand efficiency, which translated into a good physicochem. and ADMET profile. In addition, compound I [R = 1-methyl-1H-pyrazol-5-yl] was identified as an antagonist of the σ1R in view of its potent antinociceptive profile in several pain models in mice.1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

《DMSO-catalysed late-stage chlorination of (hetero)arenes》 was published in Nature Catalysis in 2020. These research results belong to Song, Song; Li, Xinyao; Wei, Jialiang; Wang, Weijin; Zhang, Yiqun; Ai, Lingsheng; Zhu, Yuchao; Shi, Xiaomeng; Zhang, Xiaohui; Jiao, Ning. Category: pyrazoles-derivatives The article mentions the following:

A highly efficient aromatic chlorination of arenes such as 1-methyl-indazole, imidazo[1,2-a]pyrazine, phenylthiophene, anthracene, etc. that is catalyzed by DMSO with N-chlorosuccinimide as the chloro source is reported. The mild conditions, easy-availability and stability of the catalyst and reagents, as well as good functional-group tolerance, showed the approach to be a versatile protocol for the late-stage aromatic chlorination of complex natural products, e.g., papaverine, drugs, e.g., diclofenac and peptides, e.g., I. The multi-gram experiment and low-cost of N-chlorosuccinimide and DMSO show great potential for drug discovery and development in industrial applications. 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: 847818-74-0Category: 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, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives

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

Electric Literature of C4H6N2OOn October 1, 2003 ,《New 1-substituted 4-cinnamoyl-5-hydroxypyrazoles and precursors thereof: Synthesis, ring closure reactions and NMR-spectroscopic investigations》 was published in Heterocycles. The article was written by Holzer, Wolfgang; Krca, Ingrid. The article contains the following contents:

Reaction of 1-substituted 5-hydroxy-1H-pyrazoles (pyrazolones) with trans-cinnamoyl chloride/calcium hydroxide in dioxane affords the corresponding 4-cinnamoyl-5-hydroxy-1H-pyrazoles. Cyclization of the latter into 5,6-dihydropyrano[2,3-c]pyrazol-4-ones proceeds in very low yields upon treatment with concentrated sulfuric acid. 1,6-Diphenyl-1H-pyrano[2,3-c]pyrazol-4-one was synthesized by reaction of 4-acetyl-5-hydroxy-1-phenyl-1H-pyrazole with benzoyl chloride and lithium bis(trimethylsilyl)amide and subsequent cyclization of the thus obtained 1,3-diketone. NMR-spectroscopic investigations with the obtained 4-substituted 5-hydroxypyrazoles and their precursors regarding their tautomeric behavior in various solvents are presented. The cyclocondensation of (2E)-1-[5-hydroxy-3-methyl-1-(phenylmethyl)-1H-pyrazol-4-yl]-3-phenyl-2-propen-1-one gave 3-methyl-6-phenyl-1-(phenylmethyl)-1H-pyrano[2,3-c]pyrazol-4-one, however in only 2% yield. In the experiment, the researchers used 2-Methyl-1H-pyrazol-3(2H)-one(cas: 3310-35-8Electric Literature of C4H6N2O)

2-Methyl-1H-pyrazol-3(2H)-one(cas: 3310-35-8) 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 C4H6N2O

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

Recommanded Product: 474432-62-7On October 8, 2020 ,《Redox-Neutral Photocatalytic C-H Carboxylation of Arenes and Styrenes with CO2》 was published in Chem. The article was written by Schmalzbauer, Matthias; Svejstrup, Thomas D.; Fricke, Florian; Brandt, Peter; Johansson, Magnus J.; Bergonzini, Giulia; Koenig, Burkhard. The article contains the following contents:

A redox-neutral CH carboxylation of arenes and styrenes using a photocatalytic approach was described for the synthesis of aryl/unsaturated-carboxylic acids RCOOH [R = 1-naphthyl, CH=CHPh, 5-cyano-2-thienyl, etc.]. Upon blue-light excitation, the anthrolate anion photocatalyst was able to reduce many aromatic compounds to their corresponding radical anions, which react with CO2 to afford carboxylic acids. High-throughput screening and computational anal. suggest that a correct balance between electron affinity and nucleophilicity of substrates was essential. This novel methodol. enabled the carboxylation of numerous aromatic compounds, including many that were not tolerated in classical carboxylation chem. Over 50 examples of CH functionalizations using CO2 or ketones illustrated a broad applicability. The experimental process involved the reaction of Pyrazolo[1,5-a]pyridine-7-carboxylic acid(cas: 474432-62-7Recommanded Product: 474432-62-7)

Pyrazolo[1,5-a]pyridine-7-carboxylic acid(cas: 474432-62-7) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 474432-62-7

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

Product Details of 52096-24-9On March 17, 2017, Kim, Og Soon; Jang, Jin Hyeok; Kim, Hyun Tae; Han, Su Jin; Tsui, Gavin Chit; Joo, Jung Min published an article in Organic Letters. The article was 《Synthesis of Fluorescent Indazoles by Palladium-Catalyzed Benzannulation of Pyrazoles with Alkynes》. The article mentions the following:

Pentasubstituted indazoles such as I (R = H, Me, t-Bu, MeO, EtO2C, F, Cl) were prepared in 34-84% yields by oxidative benzannulation reactions of pyrazoles such as 1-methylpyrazole with sym. internal alkynes such as 4-(4-RC6H4CC)C6H4R (R = H, Me, t-Bu, MeO, EtO2C, F, Cl) in the presence of Pd(OAc)2 and Cu(OAc)2 in 1,4-dioxane or by benzannulation of substituted 4-bromopyrazoles with sym. internal alkynes in the presence of Pd(OAc)2, t-Bu3P•HBF4, K2CO3, and pivalic acid in toluene; unsym. internal alkynes gave mixtures of regioisomers. 1,2-Disubstituted imidazoles also underwent oxidative benzannulation with diphenylacetylene in the presence of Pd(OAc)2 and Cu(OAc)2 in 1,4-dioxane to yield tetraphenylbenzimidazoles in 41-50% yields. The fluorescence and optical bandgaps of I (R = H, t-Bu, MeO, EtO2C, F, Cl) were determined The structure of I (R = H) was determined by X-ray crystallog. In the part of experimental materials, we found many familiar compounds, such as 1-Butyl-1H-pyrazole(cas: 52096-24-9Product Details of 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. Product Details of 52096-24-9

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

Safety of Methyl 1-methyl-1H-pyrazole-4-carboxylateOn October 6, 2017 ,《The Direct C-H Difluoromethylation of Heteroarenes Based on the Photolysis of Hypervalent Iodine(III) Reagents That Contain Difluoroacetoxy Ligands》 was published in Organic Letters. The article was written by Sakamoto, Ryu; Kashiwagi, Hirotaka; Maruoka, Keiji. The article contains the following contents:

In this letter, an efficient method for the photolytic generation of difluoromethyl radicals from [bis(difluoroacetoxy)iodo]benzene reagents is described. The present approach enables the introduction of difluoromethyl groups into various heteroarenes under mild conditions in the absence of any addnl. reagents or catalysts. 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

Product Details of 930-36-9On May 3, 2021 ,《Electrophotocatalytic C-H Azolation of Arenes》 appeared in ChemElectroChem. The author of the article were Hou, Zhong-Wei; Xu, Hai-Chao. The article conveys some information:

An electrophotocatalytic method was developed for the dehydrogenative cross coupling of arenes with azoles employing a bicatalytic system consisting of acridinium dye and (2,2,6,6-tetramethylpiperidin-1-yl)oxyl (TEMPO). The reactions were conducted in a simple undivided cell with visible-light irradiation and requires no external chem. oxidant. In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Product Details 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. Product Details of 930-36-9

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

In 2011,Guillou, Sandrine; Bonhomme, Frederic J.; Ermolenko, Mikhail S.; Janin, Yves L. published 《Simple preparations of 4 and 5-iodinated pyrazoles as useful building blocks》.Tetrahedron published the findings.Computed Properties of C4H3F3N2 The information in the text is summarized as follows:

The pyrazole nucleus has recently become a recurrent scaffold in the research fields of CropScience and oncol. We report here the preparation of an array of 4- and 5-iodinated pyrazole derivatives, such as 4-iodo-3-trifluoromethylpyrazole or Et 5-iodo-4-carboxy-3-trifluoromethylpyrazoles. This work provide access to many new pyrazole derivative, including eleven original out of sixteen iodinated building blocks, thus opening accesses to new chem. entities featuring a pyrazole nucleus.3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Computed Properties of C4H3F3N2) was used in this study.

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.Computed Properties of C4H3F3N2

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

In 2012,Rampazzi, Vincent; Massard, Alexandre; Richard, Philippe; Picquet, Michel; Le Gendre, Pierre; Hierso, Jean-Cyrille published 《A simple phosphine-diolefin-promoted copper-catalyzed N-arylation of pyrazoles with (hetero)aromatic bromides: the case of chloroarenes revisited》.ChemCatChem published the findings.Related Products of 20154-03-4 The information in the text is summarized as follows:

A molecularly defined new phosphine-diolefin cubane copper pre-catalyst used at 1.25 mol % under mild conditions promotes the coupling of pyrazoles to functionalized aryl and heteroaryl bromides, which hold a variety of functional groups. This versatile phosphorus-based system was thus successfully used, under identical conditions, for the coupling of a large scope of heteroaromatics to selectively produce pyridinyl- and pyrimidinyl-pyrazoles, as well as several novel furyl-, thienyl- and thiazolyl-substituted pyrazoles. The careful investigation of coupling with the analogous aryl and heteroaryl chlorides clearly indicated that for specifically activated chloroarenes a direct nucleophilic aromatic substitution (SNAr) is easily achieved in the absence of any copper and ligand. These results are pertinent with regards to the reported protocols in which copper-ligand systems have been claimed as useful for coupling activated chloroarenes. In the experiment, the researchers used many compounds, for example, 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