Category: pyrazoles-derivatives

《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

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 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

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 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

Related Products of 847818-74-0In 2013 ,《Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)》 appeared in Journal of Medicinal Chemistry. The author of the article were Naud, Sebastien; Westwood, Isaac M.; Faisal, Amir; Sheldrake, Peter; Bavetsias, Vassilios; Atrash, Butrus; Cheung, Kwai-Ming J.; Liu, Manjuan; Hayes, Angela; Schmitt, Jessica; Wood, Amy; Choi, Vanessa; Boxall, Kathy; Mak, Grace; Gurden, Mark; Valenti, Melanie; de Haven Brandon, Alexis; Henley, Alan; Baker, Ross; McAndrew, Craig; Matijssen, Berry; Burke, Rosemary; Hoelder, Swen; Eccles, Suzanne A.; Raynaud, Florence I.; Linardopoulos, Spiros; van Montfort, Rob L. M.; Blagg, Julian. The article conveys some information:

The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-deficient breast tumor cells are particularly dependent upon MPS1 for their survival, making it a target of significant interest in oncol. The authors report the discovery and optimization of potent and selective MPS1 inhibitors based on the 1H-pyrrolo-[3,2-c]-pyridine scaffold, guided by structure-based design and cellular characterization of MPS1 inhibition, leading to CCT251455. This potent and selective chem. tool stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding; it displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. In the experiment, the researchers used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Related Products 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, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Related Products of 847818-74-0

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