pyrazoles-derivatives

The author of 《An original class of small sized molecules as versatile fluorescent probes for cellular imaging》 were Sirbu, Doina; Diharce, Julien; Martinic, Ivana; Chopin, Nicolas; Eliseeva, Svetlana V.; Guillaumet, Gerald; Petoud, Stephane; Bonnet, Pascal; Suzenet, Franck. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Synthetic Route of C4H3F3N2 The author mentioned the following in the article:

An unusual class, compact in size, of fluorescent probes based on pyridazino-1,3a,6a-triazapentalene scaffolds exhibits promising fluorescent properties (quantum yield values up to 73%, large Stokes shifts, emission wavelengths located in the green-yellow range, excellent solubility) with good photostability suitable for optical imaging applications. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route of C4H3F3N2)

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.Synthetic Route of C4H3F3N2

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

Application of 847818-74-0In 2015 ,《Discovery and Optimization of a Porcupine Inhibitor》 appeared in Journal of Medicinal Chemistry. The author of the article were Duraiswamy, Athisayamani Jeyaraj; Lee, May Ann; Madan, Babita; Ang, Shi Hua; Tan, Eldwin Sum Wai; Cheong, Wei Wen Vivien; Ke, Zhiyuan; Pendharkar, Vishal; Ding, Li Jun; Chew, Yun Shan; Manoharan, Vithya; Sangthongpitag, Kanda; Alam, Jenefer; Poulsen, Anders; Ho, Soo Yei; Virshup, David M.; Keller, Thomas H.. The article conveys some information:

Wnt proteins regulate various cellular functions and serve distinct roles in normal development throughout life. Wnt signaling is dysregulated in various diseases including cancers. Porcupine (PORCN) is a membrane-bound O-acyltransferase that palmitoleates the Wnts and hence is essential for their secretion and function. The inhibition of PORCN could serve as a therapeutic approach for the treatment of a number of Wnt-dependent cancers. Herein, the authors describe the identification of a Wnt secretion inhibitor from cellular high throughput screening. Classical SAR based cellular optimization provided us with a PORCN inhibitor I with nanomolar activity and excellent bioavailability that demonstrated efficacy in a Wnt-driven murine tumor model. Finally, the authors also discovered that enantiomeric PORCN inhibitors show very different activity in the reporter assay, suggesting that such compounds may be useful for mode of action studies on the PORCN O-acyltransferase. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Application of 847818-74-0

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

Product Details of 847818-74-0In 2012 ,《Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Le Brazidec, Jean-Yves; Pasis, Angela; Tam, Betty; Boykin, Christina; Wang, Deping; Marcotte, Douglas J.; Claassen, Gisela; Chong, Jer-Hong; Chao, Jianhua; Fan, Junhua; Nguyen, Khanh; Silvian, Laura; Ling, Leona; Zhang, Lin; Choi, Michael; Teng, Min; Pathan, Nuzhat; Zhao, Shuo; Li, Tony; Taveras, Art. The article conveys some information:

This Letter reports the optimization of a pyrrolopyrimidine series as dual inhibitors of Aurora A/B kinases. This series is derived from a pyrazolopyrimidine series previously reported as inhibitors of aurora kinases and CDKs. In an effort to improve the selectivity of this chemotype, we switched to the pyrrolopyrimidine core which allowed functionalization on C-2. In addition, the modeling rationale was based on superimposing the structures of Aurora-A kinase and CDK2 which revealed enough differences leading to a path for selectivity improvement. The synthesis of the new series of pyrrolopyrimidine analogs relied on the development of a different route for the two key intermediates, which led to analogs with both tunable activity against CDK1 and maintained cell potency. The experimental process involved the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Product Details of 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. Product Details of 847818-74-0

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

Reference of (3-methyl-1H-pyrazol-5-yl)methanolOn September 15, 2009 ,《Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Heim-Riether, Alexander; Taylor, Steven J.; Liang, Shuang; Gao, Donghong Amy; Xiong, Zhaoming; Michael August, E.; Collins, Brandon K.; Farmer, Bennett T.; Haverty, Kathleen; Hill-Drzewi, Melissa; Junker, Hans-Dieter; Mariana Margarit, S.; Moss, Neil; Neumann, Thomas; Proudfoot, John R.; Keenan, Lana Smith; Sekul, Renate; Zhang, Qiang; Li, Jun; Farrow, Neil A.. The article contains the following contents:

Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode distinct from previously published MMP-13 inhibitors. Potency and selectivity were improved by extending the hit structure out from the active site into the S1′ pocket. In the experiment, the researchers used many compounds, for example, (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7Reference of (3-methyl-1H-pyrazol-5-yl)methanol)

(3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7) 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 (3-methyl-1H-pyrazol-5-yl)methanol

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

Application In Synthesis of 1-MethylpyrazoleOn March 31, 2022, Wang, Zhaogai; Jiang, Pengfei; Zhao, Lili; Shi, Guanying; Le, Zhang; Wang, Xiaomin; Wang, Xuzeng; Zhu, Wenkui; Prinyawiwatkul, Witoon; Xu, Zhimin published an article in International Journal of Food Science and Technology. The article was 《Concentrating sulphur-containing flavour from Toona sinensis shoots using corn oil with and without aqueous dispersion》. The article mentions the following:

Toona sinensis (TS) shoot is a seasonal and quick deteriorating vegetable with unique alliaceous flavor. In this study, corn oil was used to concentration the sulfur-containing compounds responsible for the unique TS flavor with and without aq dispersion. The level of sulfur-containing compounds in TS shoots was 0.32μg g-1 and concentratio to 2.34μg g-1 in the corn oil with aq dispersion. The sulfur-containing compounds, trans-2-Mercapto-3,4-dimethyl-2,3-dihydrothiophene and (E,Z)-Di-1-propenyldisulfide, were identified in the corn oil, while they were not detected in the oil without aq dispersion. Based on sensory and electronic nose anal., the aroma of corn oil with aq medium extraction had stronger alliaceous aroma than TS shoots and the extraction corn oil without aq dispersion. With aq dispersion assistance, the sulfur-containing aroma compounds in TS shoots were effectively concentration in corn oil. The flavor-enriched oil could serve as a flavor ingredient to deliver TS shoots aroma for different food applications. In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Application In Synthesis 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. Application In Synthesis of 1-Methylpyrazole

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

In 2015,Alexandre, Francois-Rene; Brandt, Guillaume; Caillet, Catherine; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Musiu, Chiara; Parsy, Christophe; Rahali, Houcine; Roques, Virginie; Seifer, Maria; Standring, David; Surleraux, Dominique published 《Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease》.Bioorganic & Medicinal Chemistry Letters published the findings.Synthetic Route of C4H3F3N2 The information in the text is summarized as follows:

We disclose here the synthesis of a series of macrocyclic HCV protease inhibitors, where the homoserine linked together the quinoline P2′ motif and the macrocyclic moiety. These compounds exhibit potent inhibitory activity against HCV NS3/4A protease and replicon cell based assay. Their enzymic and antiviral activities are modulated by substitutions on the quinoline P2′ at position 8 by Me and halogens and by small heterocycles at position 2. The in vitro structure activity relationship (SAR) studies and in vivo pharmacokinetic (PK) evaluations of selected compounds are described herein. In the experimental materials used by the author, we found 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route of C4H3F3N2)

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.Synthetic Route of C4H3F3N2

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

《Solubility of Water in Aprotic Heterocyclic Anion (AHA) Ionic Liquids》 was written by Avelar Bonilla, Gabriela M.; Morales-Collazo, Oscar; Brennecke, Joan F.. Product Details of 20154-03-4This research focused onwater solubility LLE aprotic tetraalkylphosphonium ionic liquid heterocyclic anion. The article conveys some information:

The hydrophobic-hydrophilic character of a series of 15 tetra-alkylphosphonium ionic liquids with aprotic heterocyclic anions (AHAs) was studied by measuring their liquid-liquid equilibrium with water. Specifically, the solubility of water in the ionic-liquid-rich phase was determined at room temperature by Karl Fischer titration The effect of the tetra-alkyl-phosphonium cation was studied by varying the alkyl chain length; as expected, hydrophobicity increases with increasing alkyl chain length. The effect of the anion was studied by pairing the tetra-alkyl-phosphonium cation with different AHAs and by adding different substituents on the anion. The anion nature, basicity, and electron withdrawing effect of different substituents proved to have a significant impact on the IL’s hydrophobicity. Changes in the alkyl chain length of the cation and the nature of the anion are able to tune the solubility of water in the ILs over an order of magnitude. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Product Details of 20154-03-4)

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.Product Details of 20154-03-4

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

In 1985,Juanes, Olga; De Mendoza, Javier; Rodriguez-Ubis, Juan Carlos published 《Synthesis of macrobicyclic ligands containing pyrazole subunits: the N,N’-bipyrazolyl cryptand》.Journal of the Chemical Society, Chemical Communications published the findings.Recommanded Product: 15366-34-4 The information in the text is summarized as follows:

The cryptands I and II were prepared in 19 and 56% yield, resp., by reaction of 3,3′-bis(bromomethyl)-1,1′-bipyrazole with anhydrous NH3 and 4,13-diaza-1,7,10,16-tetraoxacyclooctadecane, resp., in dry MeCN at 100°. The tripodal pyrazolyl ligands III (R = H, Me, CH2Ph) were prepared analogously in 35, 41, and 39% yield, resp., by reaction of the appropriate pyrazoles IV with anhydrous NH3. After reading the article, we found that the author used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Recommanded Product: 15366-34-4)

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.Recommanded Product: 15366-34-4

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

In 2016,Wucherer-Plietker, Margarita; Merkul, Eugen; Mueller, Thomas J. J.; Esdar, Christina; Knoechel, Thorsten; Heinrich, Timo; Buchstaller, Hans-Peter; Greiner, Hartmut; Dorsch, Dieter; Finsinger, Dirk; Calderini, Michel; Bruge, David; Graedler, Ulrich published 《Discovery of novel 7-azaindoles as PDK1 inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C9H15BN2O2 The information in the text is summarized as follows:

A combined screening strategy using HTS together with focused kinase library and virtual screening led to the identification of diverse chem. series as PDK1 inhibitors. The authors focused the medicinal chem. efforts on 7-azaindoles with low micromolar IC50s, e.g. I (IC50 = 1.1 μM) in the biochem. PDK1 assay. The structure-guided optimization efforts considered also PDK1 x-ray structures with weaker binding fragments and resulted in 7-azaindoles with significantly improved biochem. PDK1 potency in the two-digit nanomolar range. However, the most potent analogs only showed moderate activities in a cellular mechanistic assay, e.g. II (IC50 = 2.3 μM) together with either low microsomal stability or low permeability. The described structure-activity relationship together with PDK1 x-ray structures and early ADME data provided the basis for the subsequent hit-to-lead program. The experimental process involved the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9COA of Formula: 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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. COA of Formula: C9H15BN2O2

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

《Inhibition of the acid corrosion of iron with new pyrazole derivatives》 was written by Aouniti, A.; Hammouti, B.; Brighli, M.; Kertit, S.; Berhili, F.; El-Kadiri, S.; Ramdani, A.. Application of 29004-73-7 And the article was included in Journal de Chimie Physique et de Physico-Chimie Biologique on August 31 ,1996. The article conveys some information:

Some new synthesized pyrazole organic-type compounds have been tested as inhibitors for the corrosion of iron in 1M HCl by weight-loss and electrochem. polarization methods. Both technique gave the same order of inhibition. The compound 1,3-bis(3′-chloromethyl-5′-methyl-1′-pyrazolyl)propane (Inh.9) was the best inhibitor and its inhibition efficiency increased with increasing concentration, reaching 95% at 4.10-4M. Polarization measurements have shown that the pyrazole substances studied inhibited both the anodic reaction of iron dissolution and the cathodic reaction of hydrogen evolution. These products act without changing the mechanism of the cathodic hydrogen evolution reaction. The corrosion inhibition of pyrazole studied is regarded by a simple blocked fraction of the electrode surface related to adsorption of inhibitor species according to Langmuir isotherm model on the iron surface. The introduction in the pyrazole ring of a substitute such as -OH, -CO2H, -CO2CH3, and -Cl in the position 3, enhances the inhibiting effect of the pyrazole compounds The effect of temperature on the corrosion behavior of iron indicated that inhibition efficiencies of (Inh. 9) increased with increasing temperature in the range of 25-50°C. The apparent activation energy for iron corrosion process are modified by addition of (Inh. 9). In addition to this study using (3-methyl-1H-pyrazol-5-yl)methanol, there are many other studies that have used (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7Application of 29004-73-7) was used in this study.

(3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7) 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 29004-73-7

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