Tag: 100-200

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

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

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

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

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

In 2010,Kino, Tatsuhito; Nagase, Yu; Ohtsuka, Yuhki; Yamamoto, Kyoko; Uraguchi, Daisuke; Tokuhisa, Kenji; Yamakawa, Tetsu published 《Trifluoromethylation of various aromatic compounds by CF3I in the presence of Fe(II) compound, H2O2 and dimethyl sulfoxide》.Journal of Fluorine Chemistry published the findings.Reference of 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The trifluoromethylation of aromatic and heteroaromatic compounds by CF3I in the presence of FeSO4, H2O2 and DMSO was investigated. Various trifluoromethylated benzenes, 6-membered N-containing arenes and 5-membered heteroarenes were obtained under mild conditions. General orientation of electrophilic aromatic substitution was observed similarly as previously reported in other radical trifluoromethylations. In the experiment, the researchers used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Reference 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.Reference of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2009,Poon, Steve F.; St. Jean, David J.; Harrington, Paul E.; Henley, Charles; Davis, James; Morony, Sean; Lott, Fred D.; Reagan, Jeff D.; Lu, Jenny Ying-Lin; Yang, Yuhua; Fotsch, Christopher published 《Discovery and Optimization of Substituted 1-(1-Phenyl-1H-pyrazol-3-yl)methanamines as Potent and Efficacious Type II Calcimimetics》.Journal of Medicinal Chemistry published the findings.COA of Formula: C5H6N2O2 The information in the text is summarized as follows:

Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development of ring constrained analogs of the known calcimimetic R-568. The structure-activity relationships of various substituted heterocycles and their effects on the human calcium-sensing receptor are discussed. Pyrazole 15 (I)was shown to be efficacious in a rat in vivo pharmacodynamic model. In the part of experimental materials, we found many familiar compounds, such as 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

《Pyrazoles. VI. Electron-releasing capacity of the pyrazole ring》 was published in Journal of Heterocyclic Chemistry in 1969. These research results belong to Wijnberger, C.; Habraken, Clarisse L.. Category: pyrazoles-derivatives The article mentions the following:

Uv and 1H N.M.R. spectral data and C : O frequencies of some methylpyrazoles containing in the 3-, 4- or 5-position, a formyl-, acetyl- or ethoxycarbonyl group are reported. These data confirm earlier conclusions that, in particular, the 4-pyrazolyl group acts as an electron releasing group. The syntheses of a number of formyl-, acetyl- and ethoxycarbonyl pyrazoles are described. In addition, some 4-dicyanovinyl- and 4-tricvanovinylpyrazoles were investigated. In the experiment, the researchers used Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2Category: pyrazoles-derivatives)

Methyl 1-methyl-1H-pyrazole-4-carboxylate(cas: 5952-93-2) 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.Category: pyrazoles-derivatives

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

Category: pyrazoles-derivativesIn 1983 ,《Synthesis of 5H-pyrazolo[5,1-c][1,4]benzodiazepine》 appeared in Journal of Heterocyclic Chemistry. The author of the article were Cecchi, Lucia; Filacchioni, Guido. The article conveys some information:

Reaction of 2-O2NC6H4CH2Br with di-Me pyrazole-3,5-dicarboxylate gave di-Me 1-(2-nitrobenzyl)pyrazole-3,5-dicarboxylate which was converted in a few steps to the key intermediate oxopyrazolobenzodiazepine I. I was reduced and dehydrogenated to yield the new tricyclic system pyrazolobenzodiazepine II. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Category: pyrazoles-derivatives)

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.Category: pyrazoles-derivatives

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

Norman, Natalie J.; Bao, Si Tong; Curts, Lynne; Hui, Tiffani; Zheng, Shao-Liang; Shou, Tiffany; Zeghibe, Ana; Burdick, Izzy; Fuehrer, Hannah; Huang, Adrian published an article in 2022. The article was titled 《Highly Selective N-Alkylation of Pyrazoles: Crystal Structure Evidence for Attractive Interactions》, and you may find the article in Journal of Organic Chemistry.SDS of cas: 20154-03-4 The information in the text is summarized as follows:

Inspired by crystal structures, authors designed and achieved a catalyst-free Michael reaction for the preparation of an N1-alkyl pyrazoles I (R1 = 3-CF3, 3-COOEt, 3-NO2-4-Br, etc.; R2 = CN, COOEt) in a high yield (>90%) with excellent regioselectivity (N1/N2 > 99.9:1). The scope of this protocol has been extended to accomplish the first general regioselective N1-alkylation of 1H-pyrazoles to give di-, tri-, and tetra-substituted pyrazoles in a single step. The resulting pyrazoles bear versatile functional groups such as bromo, ester, nitro, and nitrile, offering opportunities for late-stage functionalization. This efficient methodol. will have an impact on drug discovery, as several Food and Drug Administration-approved drugs are pyrazole derivatives A working hypothesis for the regioselectivity is proposed. X-ray crystal structures of the products that highlight the attractive interactions are discussed. This report provides a rare source for the further elucidation of the attractive interactions because the isomeric ratios and the crystal structures are directly related. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4SDS of cas: 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.SDS of cas: 20154-03-4

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