pyrazoles-derivatives

Kisan Rasal, Nishant; Bhaskar Sonawane, Rahul; Vijay Jagtap, Sangeeta published their research in Chemistry & Biodiversity in 2021. The article was titled 《Synthesis, Characterization, and Biological Study of 3-Trifluoromethylpyrazole Tethered Chalcone-Pyrrole and Pyrazoline-Pyrrole Derivatives》.HPLC of Formula: 20154-03-4 The article contains the following contents:

The present study illustrates the design and synthesis of new series of 3-trifluoromethylpyrazole tethered chalcone-pyrrole and pyrazoline-pyrrole derivatives All compounds were further screened for in vitro cytostatic activities on full NCI 60 cancer cell lines at National Cancer Institute, USA. Compounds (2E)-3-(1H-pyrrol-2-yl)-1-{4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}prop-2-en-1-one (I) and (2E)-1-{3-methyl-4-[3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-3-(1H-pyrrol-2-yl)prop-2-en-1-one (II) displayed significant antiproliferative activity (Growth Percentage: -77.10 and -92.13, resp. at 10μM concentration) against the UO-31 cell lines from renal cancer and were further selected for assay at 10-fold dilutions of five different concentrations (10-4 to 10-8 M). Both compounds I and II exhibited promising antiproliferative activity (GI50: 1.36 to 0.27μM) against leukemia cancer cell lines HL-60 and RPMI-8226, colon cancer cell lines KM-12; breast cancer cell lines BT-549. Moreover, both compounds I and II were found to be non-cytotoxic (LC50>100) against HL-60, RPMI-8226, and KM-12 cell lines. Remarkably, GI50 values of these two compounds were identified as more promising than sunitinib against most cancer cell lines and in silico study of compounds I and II exemplified the desired ADME properties for drug-likeness as well as tighter interactions with VEGFR-2. Hence, compounds I and II would be good cytotoxic agents after further clin. study. The experimental process involved the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4HPLC of Formula: 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.HPLC of Formula: 20154-03-4

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

Synthetic Route of C4H3F3N2In 2015 ,《Trifluoromethylpyrazoles as anti-inflammatory and antibacterial agents: A review》 appeared in Journal of Fluorine Chemistry. The author of the article were Kaur, Kamalneet; Kumar, Vinod; Kumar Gupta, Girish. The article conveys some information:

A review. In the recent past trifluoromethylpyrazoles have gained much attention, particularly as anti-inflammatory and antibacterial agents, in the field of medicinal chem. The location of trifluoromethyl group, specially on 3- or 5-position of pyrazole nucleus, is greatly associated with variation in activity profile of the compounds Therefore, the main objective of this article is to highlight the importance of trifluoromethylpyrazoles as anti-inflammatory and antibacterial agents on a single front. The present review covers the literature from 2000 to 2015 and would certainly be proven as a great help to the medicinal chemists to explore some novel anti-inflammatory and antibacterial agents with better action profiles with minimal side effects. The experimental process involved the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route of C4H3F3N2)

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.Synthetic Route of C4H3F3N2

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

《Palladium-Phenylpyrazolylphosphine-Catalyzed Cross-Coupling of Alkenyl Pivalates》 was written by Chen, Zicong; So, Chau Ming. Name: 1-Methylpyrazole And the article was included in Asian Journal of Organic Chemistry on April 30 ,2021. The article conveys some information:

A new type of easily accessible phenylpyrazole phosphine ligand was developed. The catalyst generated from Pd(OAc)2 and PP-Phos was highly effective in the palladium-catalyzed cross-coupling of alkenyl pivalates with organomagnesium reagents. The reaction accommodated a broad scope of alkenyl carboxylates under mild conditions, providing an alternative but practical way to the synthesis of multi-substituted alkenes, e.g., I in value. After reading the article, we found that the author used 1-Methylpyrazole(cas: 930-36-9Name: 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) 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.Name: 1-Methylpyrazole

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

Electric Literature of C7H12N2On September 30, 2016 ,《Sonochemical heating profile for solvents and ionic liquid doped solvents, and their application in the N-alkylation of pyrazoles》 was published in Ultrasonics Sonochemistry. The article was written by Frizzo, Clarissa P.; Bacim, Carolini; Moreira, Dayse N.; Rodrigues, Leticia V.; Zimmer, Georgia C.; Bonacorso, Helio G.; Zanatta, Nilo; Martins, Marcos A. P.. The article contains the following contents:

The heating profile for 25 solvents was determined in ultrasonic probe equipment at amplitudes of 20%, 25%, and 30%. Each solvent was heated in accordance with its b.p. The effect of vapor pressure, surface tension, and viscosity of the solvents in dissipated ultrasonic power (Up) was evaluated. Multiple regression anal. of these solvent properties and dissipated Up revealed that solvent viscosity was the property that most strongly affected dissipated Up. Experimentation involving acetonitrile doped with [BMIM][BF4] indicated faster heating than MeCN. Aprotic polar solvents such as DMSO, DMF, and MeCN were tested in the N-alkylation of pyrazoles under ultrasonic conditions. After 5 min at 90°, the reactants were totally converted into product in these solvents. Solvents, with low dissipated Up (e.g., toluene) were tested. Conversions were lower compared to those of aprotic polar solvents. When the reactions were done in hexane, no conversion to product was observed To check the effect of doping in solvents with low Up, [BMIM][BF4], DMSO, and DMF were selected. The conversions for toluene doped with [BMIM][BF4], DMSO, and DMF were 100%, 59%, and 25%, resp. These conversions were greater than when done in just toluene (46%). Thus, [BMIM][BF4] was the best polar doping solvent, followed by DMSO. DMF was not considered to be a satisfactory doping solvent. No conversion was observed for reactions in the absence of base performed in DMSO, DMF, and MeCN doped with [BMIM][BF4]. The experimental process involved 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 In Synthesis of 1-Butyl-1H-pyrazoleOn October 22, 2018 ,《Pyrazolium Ionic Liquid Co-catalysts for the Electroreduction of CO2》 was published in ACS Applied Energy Materials. The article was written by Vasilyev, Dmitry; Shirzadi, Erfan; Rudnev, Alexander V.; Broekmann, Peter; Dyson, Paul J.. The article contains the following contents:

Pyrazolium ionic liquids (Pz ILs) were employed as co-catalysts for electrochem. conversion of CO2 to CO on a Ag disk electrode, leading to a significant decrease in the onset potential for the reduction (∼500 mV). The electrochem. conversion of CO2 to CO proceeds in MeCN-based electrolytes containing Pz IL co-catalysts with faradaic efficiencies (FEs) of nearly 100% over a range of at least 0.5 V, and the Pz cations remain intact over prolonged CO2 electrolysis. The impact of alkyl substituents on the Pz ring and the influence of H2O on the process are also discussed. After reading the article, we found that the author used 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

Reference of 1-MethylpyrazoleOn November 30, 2019 ,《Catalyst-free addition of secondary phosphine chalcogenides to pyrazolecarbaldehydes》 appeared in Mendeleev Communications. The author of the article were Malysheva, Svetlana F.; Kuimov, Vladimir A.; Belogorlova, Natalia A.; Gusarova, Nina K.; Taydakov, Ilya V.; Albanov, Alexander I.; Eremenko, Igor L.; Trofimov, Boris A.. The article conveys some information:

(Chalcogenophosphoryl)hydroxymethyl-substituted pyrazoles were obtained by catalyst-free reaction between 4- and 5-pyrazolecarbaldehydes and secondary phosphine chalcogenides R2P(X)H [R = Ph, (CH2)2Ph, X = O, S, Se] at 23-50° in toluene. In the experiment, the researchers used many compounds, for example, 1-Methylpyrazole(cas: 930-36-9Reference 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. Reference of 1-Methylpyrazole

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

Caliskan, Burcu; Yilmaz, Akin; Evren, Ilker; Menevse, Sevda; Uludag, Orhan; Banoglu, Erden published an article on February 28 ,2013. The article was titled 《Synthesis and evaluation of analgesic, anti-inflammatory, and anticancer activities of new pyrazole-3(5)-carboxylic acid derivatives》, and you may find the article in Medicinal Chemistry Research.Name: Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate The information in the text is summarized as follows:

1-Benzyl-5(3)-p-tolyl-1H-pyrazole-3(5)-carboxylic acid derivatives were prepared and characterized by IR, 1H NMR, and mass spectroscopy. Compounds were evaluated for their in vivo analgesic and anti-inflammatory activity using the p-benzoquinone-induced writhing test and the carrageenan-induced paw edema model, resp. Out of 14 compounds tested, exhibited potent analgesic and/or anti-inflammatory activity as compared to reference drugs aspirin and indomethacin. Anticancer activity of these compounds was assessed against five cancer cell lines with the MTT assay (HL-60, human promyelocytic leukemia cells; HeLa, human cervical cancer cells; Raji, human B lymphocyte cell line; MCF7, human breast adenocarcinoma cell line; MDA-MB-231, estrogen-independent human breast cancer cell line). Three compounds with high anti-inflammatory activity, and also two compounds with mild anti-inflammatory activity exhibited promising anticancer activity against some selected cell lines. In addition to this study using Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate, there are many other studies that have used Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Name: Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate) was used in this study.

Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) 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. Name: Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate

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

In 2012,Journal of Biological Chemistry included an article by Kroth, Heiko; Ansaloni, Annalisa; Varisco, Yvan; Jan, Asad; Sreenivasachary, Nampally; Rezaei-Ghaleh, Nasrollah; Giriens, Valerie; Lohmann, Sophie; Lopez-Deber, Maria Pilar; Adolfsson, Oskar; Pihlgren, Maria; Paganetti, Paolo; Froestl, Wolfgang; Nagel-Steger, Luitgard; Willbold, Dieter; Schrader, Thomas; Zweckstetter, Markus; Pfeifer, Andrea; Lashuel, Hilal A.; Muhs, Andreas. Recommanded Product: 192701-73-8. The article was titled 《Discovery and Structure Activity Relationship of Small Molecule Inhibitors of Toxic β-Amyloid-42 Fibril Formation》. The information in the text is summarized as follows:

Increasing evidence implicates Aβ peptides self-assembly and fibril formation as crucial events in the pathogenesis of Alzheimer disease. Thus, inhibiting Aβ aggregation, among others, has emerged as a potential therapeutic intervention for this disorder. Herein, we employed 3-aminopyrazole as a key fragment in our design of non-dye compounds capable of interacting with Aβ42 via a donor-acceptor-donor hydrogen bond pattern complementary to that of the β-sheet conformation of Aβ42. The initial design of the compounds was based on connecting two 3-aminopyrazole moieties via a linker to identify suitable scaffold mols. Addnl. aryl substitutions on the two 3-aminopyrazole moieties were also explored to enhance π-π stacking/hydrophobic interactions with amino acids of Aβ42. The efficacy of these compounds on inhibiting Aβ fibril formation and toxicity in vitro was assessed using a combination of biophys. techniques and viability assays. Using structure activity relationship data from the in vitro assays, we identified compounds capable of preventing pathol. self-assembly of Aβ42 leading to decreased cell toxicity. In the experiment, the researchers used many compounds, for example, Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Recommanded Product: 192701-73-8)

Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) 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: 192701-73-8

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

O’Sullivan, Leonie; Patel, Ketul V.; Rowley, Ben C.; Brownsey, Duncan K.; Gorobets, Evgueni; Gelfand, Benjamin S.; Van Humbeck, Jeffrey F.; Derksen, Darren J. published an article on January 7 ,2022. The article was titled 《Regioselective Synthesis of C3-Hydroxyarylated Pyrazoles》, and you may find the article in Journal of Organic Chemistry.Product Details of 930-36-9 The information in the text is summarized as follows:

The first regioselective route to C3-hydroxyarylated pyrazoles obtained through reaction of pyrazole N-oxides with arynes using mild conditions is reported. Importantly, this method does not require the C4 and C5 positions of the pyrazole to be functionalized to observe regioselectivity. Using this method, authors completed the synthesis of a recently reported JAK 1/2 inhibitor. Authors’ synthesis produces the desired product in 4 steps from com. available starting materials. The results came from multiple reactions, including the reaction of 1-Methylpyrazole(cas: 930-36-9Product Details of 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. Product Details of 930-36-9

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

The author of 《3-Methyl-5-carboxamidopyrazole, a long-lasting inhibitor of lipolysis》 were Bizzi, Adalgisa; Codegoni, A. M.; Garattini, Silvio. And the article was published in Farmaco, Edizione Scientifica in 1967. Related Products of 29004-73-7 The author mentioned the following in the article:

Nineteen 3-methyl-5-carboxypyrazole (I) derivatives were tested orally in rats for their capacity to lower plasma free fatty acids. Esterification or the reduction of the carboxy radical did not affect the properties of I; the presence of N1-substituted Me or benzyl reduced the lipolytic effect. 3-Methyl-5-carboxamidopyrazole (II) was the longest lasting compound II prevented and counteracted the increased deposition of liver triglycerides induced by ACTH (200 I.U./kg., given s.c.) or 50% EtOH (16 ml./kg.) and it reduced the plasma ketone body concentration in fasted animals. 16 references. After reading the article, we found that the author used (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7Related Products of 29004-73-7)

(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. Related Products of 29004-73-7

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