Category: 15366-34-4

Category: pyrazoles-derivativesIn 2017 ,《Novel pyrazolo[1,5-a]pyridines as orally active EP1 receptor antagonists: Synthesis, structure-activity relationship studies, and biological evaluation》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Umei, Kentaro; Nishigaya, Yosuke; Kondo, Atsushi; Tatani, Kazuya; Tanaka, Nobuyuki; Kohno, Yasushi; Seto, Shigeki. The article conveys some information:

Novel pyrazolo[1,5-a]pyridine derivatives were designed, synthesized and evaluated as orally active EP1 antagonists for the treatment of overactive bladder. Matched mol. pair anal. (MMPA) allowed the design of a new series of pyrazolo[1,5-a]pyridine derivatives Structure-activity relationships (SAR) studies of were performed, leading to identification of the nanomolar-level EP1 antagonist I, which exhibited good pharmacol. effect through intraduodenal (id) administration in a 17-phenyltrinor prostaglandin E2-induced bladder contraction model in rats. The experimental part of the paper was very detailed, including the reaction process of 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

Recommanded Product: 15366-34-4In 2010 ,《Synthesis and evaluation of the anti-inflammatory properties of selenium-derivatives of celecoxib》 was published in Chemico-Biological Interactions. The article was written by Desai, Dhimant; Kaushal, Naveen; Gandhi, Ujjawal H.; Arner, Ryan J.; D’Souza, Christopher; Chen, Gang; Vunta, Hema; El-Bayoumy, Karam; Amin, Shantu; Prabhu, K. Sandeep. The article contains the following contents:

Celecoxib is a selective cyclooxygenase (COX)-2 inhibitor used to treat inflammation, while selenium is known to down-regulate the transcription of COX-2 and other pro-inflammatory genes. To expand the anti-inflammatory property, wherein celecoxib could inhibit pro-inflammatory gene expression at extremely low doses, we incorporated selenium (Se) into two Se-derivatives of celecoxib, namely; selenocoxib-2 and selenocoxib-3. In vitro kinetic assays of the inhibition of purified human COX-2 activity by these compounds indicated that celecoxib and selenocoxib-3 had identical K I values of 2.3 and 2.4 μM; while selenocoxib-2 had a lower K I of 0.72 μM. Furthermore, selenocoxib-2 inhibited lipopolysaccharide-induced activation of NF-κB leading to the down-regulation of expression of COX-2, iNOS, and TNFα more effectively than selenocoxib-3 and celecoxib in RAW264.7 macrophages and murine bone marrow-derived macrophages. Studies with rat liver microsomes followed by UPLC-MS-MS anal. indicated the formation of selenenylsulfide conjugates of selenocoxib-2 with N-acetylcysteine. Selenocoxib-2 was found to release minor amounts of Se that was effectively inhibited by the CYP inhibitor, sulphaphenazole. While these studies suggest that selenocoxib-2, but not celecoxib and selenocoxib-3, targets upstream events in the NF-κB signaling axis, the ability to effectively suppress NF-κB activation independent of cellular selenoprotein synthesis opens possibilities for a new generation of COX-2 inhibitors with significant and broader anti-inflammatory potential. In the part of experimental materials, we found many familiar compounds, such as 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. 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.Recommanded Product: 15366-34-4

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

In 2010,Forster, Laura; Ludwig, Joachim; Kaptur, Martina; Bovens, Stefanie; Elfringhoff, Alwine Schulze; Holtfrerich, Angela; Lehr, Matthias published 《1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase》.Bioorganic & Medicinal Chemistry published the findings.Application of 15366-34-4 The information in the text is summarized as follows:

Cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH) are enzymes, which have emerged as attractive targets for the development of analgetic and anti-inflammatory drugs. We recently reported that 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid (10) and related compounds are inhibitors of cPLA2α. Since cPLA2α and FAAH possess several common structural features, we now screened this substance series together with some new derivatives for FAAH inhibition. Some of the assayed compounds proved to be selective cPLA2α inhibitors, while others showed high FAAH and moderate cPLA2α inhibitory potency. Furthermore, several derivatives were favorably active against both enzymes and, therefore, could represent agents, which have improved analgetic and anti-inflammatory qualities in comparison with selective cPLA2α and FAAH inhibitors. In the experiment, the researchers used many compounds, for example, Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Application of 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.Application of 15366-34-4

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

In 2017,Bezencon, Olivier; Heidmann, Bibia; Siegrist, Romain; Stamm, Simon; Richard, Sylvia; Pozzi, Davide; Corminboeuf, Olivier; Roch, Catherine; Kessler, Melanie; Ertel, Eric A.; Reymond, Isabelle; Pfeifer, Thomas; de Kanter, Ruben; Toeroek-Schafroth, Michael; Moccia, Luca G.; Mawet, Jacques; Moon, Richard; Rey, Markus; Capeleto, Bruno; Fournier, Elvire published 《Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies》.Journal of Medicinal Chemistry published the findings.Quality Control of Methyl 1H-pyrazole-3-carboxylate The information in the text is summarized as follows:

The authors report the discovery and pharmacol. characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be neg. in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478 (N-(1-((5-cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide)), which has been selected as a clin. candidate. In the experiment, the researchers used many compounds, for example, Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Quality Control of Methyl 1H-pyrazole-3-carboxylate)

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.Quality Control of Methyl 1H-pyrazole-3-carboxylate

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

HPLC of Formula: 15366-34-4In 1995 ,《4-Methoxybenzyl, a versatile protecting group for the regiospecific lithiation and functionalization of pyrazoles》 appeared in Synthetic Communications. The author of the article were Subramanyam, Chakrapani. The article conveys some information:

The use of the 4-methoxybenzyl protecting group for the regiospecific metalation/functionalization of pyrazole was reported. The protection of 1H-pyrazole gave 1-[(4-methoxyphenyl)methyl]-1H-pyrazole which underwent regioselective lithiation to give 5-lithio-1-[(4-methoxyphenyl)methyl]-1H-pyrazole. Treatment of the latter with Et N-methoxy-N-methylcarbamate gave di-[1-[(4-methoxyphenyl)methyl]-1H-pyrazol-5-yl] methanone. Deprotection of the latter gave the desired di(1H-pyrazol-3-yl) methanone.Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4HPLC of Formula: 15366-34-4) was used in this study.

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.HPLC of Formula: 15366-34-4

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

Polina, Saibabu; Putta, V. P. Rama Kishore; Gujjarappa, Raghuram; Pujar, Prasad Pralhad; Malakar, Chandi C. published their research in Journal of Heterocyclic Chemistry in 2021. The article was titled 《Aza-Michael addition of 1,2-diazoles to structurally diverse enones: Efficient methods toward β-amino ketones》.COA of Formula: C5H6N2O2 The article contains the following contents:

An efficient and mild protocol was realized using 1,2-diazoles and related heterocycles with cyclic and acyclic enones in presence of T3P (2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphorinane-2,4,6-trioxide) toward the regioselective formation of N-cycloalkyl heterocycles at room temperature The developed reaction conditions showcased good selectivity over a wide range of 1,2-diazoles and enones by delivering N-cycloalkyl heterocycles in excellent yields. In the experiment, the researchers used many compounds, for example, 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

Formula: C5H6N2O2In 1994 ,《Thermal and photochemical evolution of triazolines obtained by addition of diazo compounds to methyl esters of oximino-malonodinitriles, oximino-cyanoacetates and oximino-malonates》 was published in Canadian Journal of Chemistry. The article was written by Perrocheau, Jacques; Carrie, Robert; Fleury, Jean-Pierre. The article contains the following contents:

Thermolysis of 1,2,3-triazolines I [R = Ts, COC6H4Z-4, Ac; R1 = H, Me, Ph, (MeO)2CH] leads to the corresponding aziridines only when X = Y = CO2Me, and then with a very low yield. However, photolysis or evolution in the presence of trifluoroacetic acid gives good results when carried out at sufficiently low temperature The thermolysis study of I shows a new route to 1,2,3-triazoline decomposition that has not yet been mentioned in the literature. The easy elimination of the p-toluenesulfonate or benzoate group explains this particular behavior. The experimental part of the paper was very detailed, including the reaction process of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Formula: C5H6N2O2)

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.Formula: C5H6N2O2

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

《Synthesis of 2,2,2-trifluoroethyl 1H-pyrazole carboxylates: Insight into the mechanism of trichloromethyl group hydrolysis》 was written by Goncalves, Helena A.; Pereira, Bruna A.; Teixeira, Wystan K. O.; Moura, Sidnei; Flores, Darlene C.; Flores, Alex F. C.. HPLC of Formula: 15366-34-4This research focused ontrichloro methoxyalkenone trifluoroethanol cyclocondensation hydrolysis; methyl pyrazole carboxylate trifluoroethyl pyrazole carboxylate preparation green chem; trifluoroethanol trichloro hydroxyalkenone cyclocondensation; trifluoroethyl pyrazole carboxylate preparation green chem. The article conveys some information:

One-pot synthesis of 2,2,2-trifluoroethyl 1H-pyrazole-5(3)-carboxylates and via cyclocondensation of 1,1,1-trichloro-4-alkoxy-3-alken-2-ones, 1,1,1-trichloro-2,4-alkanediones and 1-aryl-4,4,4-trichloro-1,3-butanediones with hydrazine hydrochloride in 2,2,2-trifluoroethanol (TFE) was reported. Considering the low nucleophilicity of TFE in relation to methanol or ethanol, the results provided evidence for the mechanism of hydrolysis of the trichloromethyl group attached to the 1H-pyrazol ring. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4HPLC of Formula: 15366-34-4)

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.HPLC of Formula: 15366-34-4

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

Product Details of 15366-34-4In 2022 ,《Discovery and Optimization of Highly Selective Inhibitors of CDK5》 was published in Journal of Medicinal Chemistry. The article was written by Daniels, Matthew H.; Malojcic, Goran; Clugston, Susan L.; Williams, Brett; Coeffet-Le Gal, Marie; Pan-Zhou, Xin-Ru; Venkatachalan, Srinivasan; Harmange, Jean-Christophe; Ledeboer, Mark. The article contains the following contents:

Autosomal dominant polycystic kidney disease (ADPKD) is the most prevalent monogenic human disease, but to date, only one therapy (tolvaptan) is approved to treat kidney cysts in ADPKD patients. Cyclin-dependent kinase 5 (CDK5), an atypical member of the cyclin-dependent kinase family, has been implicated as a target for treating ADPKD. However, no compounds have been disclosed to date that selectively inhibit CDK5 while sparing the broader CDK family members. Herein, we report the discovery of CDK5 inhibitors, including GFB-12811 (I), that are highly selective over the other tested kinases. In cellular assays, our compounds demonstrate CDK5 target engagement while avoiding anti-proliferative effects associated with inhibiting other CDKs. In addition, we show that the compounds in this series exhibit promising in vivo PK profiles, enabling their use as tool compounds for interrogating the role of CDK5 in ADPKD and other diseases. After reading the article, we found that the author used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Product Details of 15366-34-4)

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.Product Details of 15366-34-4

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