Day: October 19, 2022

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

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 2014,Huang, Qinhua; Johnson, Ted W.; Bailey, Simon; Brooun, Alexei; Bunker, Kevin D.; Burke, Benjamin J.; Collins, Michael R.; Cook, Andrew S.; Cui, J. Jean; Dack, Kevin N.; Deal, Judith G.; Deng, Ya-Li; Dinh, Dac; Engstrom, Lars D.; He, Mingying; Hoffman, Jacqui; Hoffman, Robert L.; Johnson, Patrick S.; Kania, Robert S.; Lam, Hieu; Lam, Justine L.; Le, Phuong T.; Li, Qiuhua; Lingardo, Laura; Liu, Wei; Lu, Melissa West; McTigue, Michele; Palmer, Cynthia L.; Richardson, Paul F.; Sach, Neal W.; Shen, Hong; Smeal, Tod; Smith, Graham L.; Stewart, Albert E.; Timofeevski, Sergei; Tsaparikos, Konstantinos; Wang, Hui; Zhu, Huichun; Zhu, Jinjiang; Zou, Helen Y.; Edwards, Martin P. published 《Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib》.Journal of Medicinal Chemistry published the findings.SDS of cas: 847818-74-0 The information in the text is summarized as follows:

Crizotinib, an anaplastic lymphoma kinase (ALK) receptor tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration in 2011, is efficacious in ALK and ROS pos. patients. Under pressure of crizotinib treatment, point mutations arise in the kinase domain of ALK, resulting in resistance and progressive disease. The successful application of both structure-based and lipophilic-efficiency-focused drug design resulted in aminopyridine (I), which was potent across a broad panel of engineered ALK mutant cell lines and showed suitable preclin. pharmacokinetics and robust tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M). After reading the article, we found that the author used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0SDS of cas: 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. SDS of cas: 847818-74-0

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

In 2017,King, Dalton; Iwuagwu, Christiana; Cook, Jim; McDonald, Ivar M.; Mate, Robert; Zusi, F. Christopher; Hill, Matthew D.; Fang, Haiquan; Zhao, Rulin; Wang, Bei; Easton, Amy E.; Miller, Regina; Post-Munson, Debra; Knox, Ronald J.; Gallagher, Lizbeth; Westphal, Ryan; Molski, Thaddeus; Fan, Jingsong; Clarke, Wendy; Benitex, Yulia; Lentz, Kimberley A.; Denton, Rex; Morgan, Daniel; Zaczek, Robert; Lodge, Nicholas J.; Bristow, Linda J.; Macor, John E.; Olson, Richard E. published 《BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia》.ACS Medicinal Chemistry Letters published the findings.HPLC of Formula: 847818-74-0 The information in the text is summarized as follows:

The therapeutic treatment of neg. symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclin. literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provide an effective approach to treating cognitive dysfunction in schizophrenia. The authors report herein the discovery and evaluation of I (BMS-933043), a novel and potent α7 nACh receptor partial agonist with high selectivity against other nicotinic acetylcholine receptor subtypes (>100-fold) and the 5-HT3A receptor (>300-fold). In vivo activity was demonstrated in a preclin. model of cognitive impairment, mouse novel object recognition. BMS-933043 has completed Phase I clin. trials.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) 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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. HPLC of Formula: 847818-74-0

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

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