Tag: M.W=100-150

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Category: pyrazoles-derivatives.

Zak, Mark;Hanan, Emily J.;Lupardus, Patrick;Brown, David G.;Robinson, Colin;Siu, Michael;Lyssikatos, Joseph P.;Romero, F. Anthony;Zhao, Guiling;Kellar, Terry;Mendonca, Rohan;Ray, Nicholas C.;Goodacre, Simon C.;Crackett, Peter H.;McLean, Neville;Hurley, Christopher A.;Yuen, Po-wai;Cheng, Yun-Xing;Liu, Xiongcai;Liimatta, Marya;Kohli, Pawan Bir;Nonomiya, Jim;Salmon, Gary;Buckley, Gerry;Lloyd, Julia;Gibbons, Paul;Ghilardi, Nico;Kenny, Jane R.;Johnson, Adam research published 《 Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling》, the research content is summarized as follows. Disruption of interleukin-13 (IL-13) signaling with large mol. antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor complex, JAK inhibition may offer an alternate small mol. approach to disrupting IL-13 signaling. Herein we demonstrate that JAK1 is likely the isoform most important to IL-13 signaling. Structure-based design was then used to improve the JAK1 potency of a series of previously reported JAK2 inhibitors. The ability to impede IL-13 signaling was thereby significantly improved, with the best compounds exhibiting single digit nM IC₅₀‘s in cell-based assays dependent upon IL-13 signaling. Appropriate substitution was further found to influence inhibition of a key off-target, LRRK2. Finally, the most potent compounds were found to be metabolically labile, which makes them ideal scaffolds for further development as topical agents for IL-13 mediated diseases of the lungs and skin (for example asthma and atopic dermatitis, resp.).

Category: pyrazoles-derivatives, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Synthetic Route of 2075-46-9.

Zakharov, V. V.;Chukanov, N. V.;Zyuzin, I. N.;Nedel’ko, V. V.;Korsunskii, B. L. research published 《 Thermal Decomposition of N-[2,2-Bis(methoxy-NNO-azoxy)ethyl]-4-Nitropyrazole》, the research content is summarized as follows. The thermal decomposition of high-energy N-[2,2-bis(methoxy-NNO-azoxy)ethyl]-4-nitropyrazole is studied and the composition of the products formed is determined using differential scanning calorimetry, thermogravimetry, mass spectrometry, and IR spectroscopy. Its heat of melting, as well as the heat and energy of activation and the preexponential factor for its thermal decomposition, have been determined The mechanism of the process is discussed. It is shown that introducing a nitropyrazole fragment into a diazene oxide mol. does not lead to a decrease in its thermal stability.

Synthetic Route of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. COA of Formula: C3H3N3O2.

Zalaru, Christina;Dumitrascu, Florea;Draghici, Constantin;Tarcomnicu, Isabela;Tatia, Rodica;Moldovan, Lucia;Chifiriuc, Mariana-Carmen;Lazar, Veronica;Marinescu, Maria;Nitulescu, Mihai George;Ferbinteanu, Marilena research published 《 Synthesis, spectroscopic characterization, DFT study and antimicrobial activity of novel alkylaminopyrazole derivatives》, the research content is summarized as follows. A new series of substituted N,N-bis-[(1H-pyrazol-1-yl)methyl]aminohexadecane Mannich bases I (R = H, CH₃; R¹ = H, I, NO₂) were synthesized, characterized by IR, ¹H NMR ¹³C NMR, UV-Vis, MS and elemental anal., and tested for their biol. activity. All the synthesized compounds were tested for in vitro antimicrobial activity against a panel of selected bacterial and fungal strains using erythromycin and clotrimazole as standards Most of the synthesized compounds demonstrated very good activity at min. inhibitory concentrations (MICs). Compound I (R = H, R¹ = I) with an halogen atom into the pharmacophore structure exhibited the most significant activity against Bacillus subtilis (MIC = 0.007 μgmL^-1) vs. erythromycin as standard In vitro cytotoxicity of the new compounds was studied using MTT assay. The anal. of the test cells showed that the newly synthesized alkylaminopyrazoles were biocompatible until a concentration of 5 μgmL^-1; two compounds presented a high degree of biocompatibility on the studied concentration range.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., COA of Formula: C3H3N3O2

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Synthetic Route of 37622-90-5.

Zhang, Jin;Jia, Run-Ping;Wang, Dong-Hui research published 《 Copper-catalyzed C-N cross-coupling of arylboronic acids with N-acylpyrazoles》, the research content is summarized as follows. A copper-catalyzed C-N bond forming reaction of arylboronic acids and N-acylpyrazoles was developed. This procedure used N-acetyl protected pyrazoles as starting material instead of free pyrazoles (NH). The reaction worked under neutral conditions and did not require any base or ligand. The reaction showed good functional group tolerance.

Synthetic Route of 37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, 37622-90-5.

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Name: Ethyl 4-pyrazolecarboxylate.

Zhang, Xiaoxiang;Yu, Wenhua;Nie, Yiyu;Zhang, Yingying;Gu, Xiaoting;Wei, Wanxing;Zhang, Zhuan;Liang, Taoyuan research published 《 Copper-iodine co-catalyzed C-H aminoalkenylation of indoles via temperature-controlled selectivity switch: facile synthesis of 2-azolyl-3-alkenylindoles》, the research content is summarized as follows. An efficient copper-iodine co-catalyzed 2,3-difunctionalization of indoles with azoles and phenols via temperature-controlled selectivity switch has been developed for the green synthesis of 2-azolyl-3-alkenylindoles. The strategy involves the simultaneous establishment of C-C and C-N bonds in one single operation and provides straightforward access to a wide range of functionalized indoles with high regio-selectivity and good functional group compatibility. The utility of the new protocol was demonstrated by the concise synthesis of the analog of a potent anticancer agent. This work paves the way for further innovative direct difunctionalization of carbon-carbon double bonds.

37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, Name: Ethyl 4-pyrazolecarboxylate

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Quality Control of 2075-46-9.

Zhang, Yanmin;Chen, Yadong;Zhang, Danfeng;Wang, Lu;Lu, Tao;Jiao, Yu research published 《 Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines》, the research content is summarized as follows. Computational and exptl. studies were applied to the discovery of a series of novel vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors. Eight compounds exhibited nanomolar IC₅₀ values against VEGFR-2, and compounds 6, 19, 22, and 23 showed potent antiproliferative effects against several cell lines. Particularly, compound 23 behaved better than FDA approved drugs, sorafenib and sunitinib, in antiproliferative activity against cell lines related to all nine tumor types tested (GI₅₀ values), and it was better or comparable in safety (LC₅₀ values). Compound 23 even demonstrated a high potency on one of the drug-resistant cell lines (NCI/ADR-RES) responsible for ovarian cancer and cell lines contributing to prostate cancer, regarded as one of the VEGF/VEGFR pathway drug-resistant tumors. This compound is likely a promising candidate for the treatment of leukemia, non-small cell lung cancer (NSCLC), colon cancer, ovarian cancer, and breast cancer with a suitable balance of both efficacy and safety.

Quality Control of 2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., 2075-46-9.

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

Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Related Products of 2075-46-9.

Xiao, Daipeng;He, Fen;Peng, Dongming;Zou, Min;Peng, Junying;Liu, Pan;Liu, Yanfei;Liu, Zhenbao research published 《 Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives》, the research content is summarized as follows. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The mol. docking study was carried out in mol. operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, mol. docking anal. showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from mol. interaction aspect.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Related Products of 2075-46-9

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 37622-90-5, formula is C6H8N2O2, Name is Ethyl 4-pyrazolecarboxylate. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. Synthetic Route of 37622-90-5.

Xie, Shihua;Wang, Hui;Wang, Yong;Yang, Qifan;Zhu, Hongjun research published 《 Visible-light-induced Catalyzed Dehydrogenative Coupling of Quinoxalin-2(1H)-ones with Azoles Using Carbon Nitride》, the research content is summarized as follows. An efficient visible-light-induced catalyzed dehydrogenative coupling of quinoxalin-2(1H)-ones with azoles was developed, a protocol that did not require prefunctionalization of the substrates and produced hydrogen (H₂). Meanwhile, this reaction proceeded without the addition of other metal and oxidant and provided a broad range of 3-aminoquinoxalin-2(1H)-ones in medium to good yield. Furthermore, this protocol provided advantages of easy and simple operation, high chemoselectivity and a recyclable catalyst. A preliminary mechanistic investigation revealed that the reaction involved a radical process.

Synthetic Route of 37622-90-5, Ethyl 4-pyrazolecarboxylate, also known as Ethyl pyrazole-4-carboxylate, is a useful research compound. Its molecular formula is C6H8N2O2 and its molecular weight is 140.14 g/mol. The purity is usually 95%.

Ethyl pyrazole-4-carboxylate is a low yield, transition metal salt that is used in the synthesis of pyrazoles. It can be synthesized by the reaction of sodium ethoxide with ethyl chloroformate and a Grignard reagent. Sodium ethoxide is added to a suspension of sodium chloride and dried ethyl chloroformate, followed by addition of magnesium turnings. The mixture is refluxed for one hour, cooled, and filtered to give crystals. Ethyl pyrazole-4-carboxylate is used in the preparation of ethyl esters from aliphatic alcohols by reacting with boron trichloride or phosphorus pentachloride. It participates in certain chemical reactions as a byproduct and can damage equipment during chemical reactions. The yield of this compound can be increased by using an excess amount of Grignard reagent or adding hexamethylenetetramine to the reaction mixture, 37622-90-5.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Computed Properties of 2075-46-9.

Xu, Jun;Du, Kui;Shen, Jiabin;Shen, Chao;Chai, Kejie;Zhang, Pengfei research published 《 Copper(II)-Catalyzed Selective Para Amination of Arylamine with Pyrazole by C-H Functionalization》, the research content is summarized as follows. A coordinating activation strategy for selective para amination of arylamine with pyrazole is developed. Various substrates are compatible, giving the corresponding products in moderate to good yields. This strategy provides a practical solution for the efficient synthesis of arylamine-containing pharmacophores from simple starting materials. A single electron transfer mechanism is suggested for this reaction.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., Computed Properties of 2075-46-9

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

Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 1-Methyl-5-(trifluoromethyl)pyrazole underwent deprotonation and subsequent carboxylation mainly or exclusively at either the 4-position of the heterocycle or at the nitrogen-attached methyl group. COA of Formula: C3H3N3O2.

Xu, Pengfei;Shen, Pei;Wang, Hai;Qin, Lian;Ren, Jie;Sun, Qiushuang;Ge, Raoling;Bian, Jinlei;Zhong, Yi;Li, Zhiyu;Wang, JuBo;Qiu, Zhixia research published 《 Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2》, the research content is summarized as follows. Herein,the design, synthesis, and structure-activity relationships of a series of imidazopyrrolopyridines derivatives I [R¹ = H, cyclopropyl, 2-chlorophenyl, etc.; R2 = cyanomethyl, 4,4,4-trifluorobutyl, (3-(cyanomethyl)-1-ethylsulfonyl-azetidin-3-yl), etc.] that selectively inhibit Janus kinase 2 (JAK2) was described . These screening cascades revealed that I [R¹ = H; R² = 3-cyanopropyl] was a preferred compound, with IC₅₀ values of 10 nM for JAK2. Moreover, I [R¹ = H; R² = 3-cyanopropyl] was a selective JAK2 inhibitor with 19-fold, >30-fold and >30-fold selectivity over JAK1, JAK3 and TYK2 resp. In cytokine-stimulated cell-based assays, I [R¹ = H; R² = 3-cyanopropyl] exhibited a higher JAK2 selectivity over JAK1 isoforms. Indeed, at a dose of 20 mg/kg compound I [R¹ = H; R² = 3-cyanopropyl], pSTAT3 and pSTAT5 expression was reduced to levels comparable to those of control animals untreated with GM-CSF. Addnl., I [R¹ = H; R² = 3-cyanopropyl] showed a relatively good bioavailability (F = 38%), a suitable half-life time (T1/2 = 1.9 h), a satisfactory metabolic stability, suggesting that I [R¹ = H; R² = 3-cyanopropyl] might be a promising inhibitor of JAK2 for further development research for the treatment of MPNs.

2075-46-9, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g/mol. The purity is usually 95%.

4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson’s disease., COA of Formula: C3H3N3O2

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