Category: 761446-44-0

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Product Details of C10H17BN2O2.

Rodriguez, Diana;Maneiro, Maria;Vazquez-Ucha, Juan C.;Beceiro, Alejandro;Gonzalez-Bello, Concepcion research published 《 6-Arylmethylidene Penicillin-Based Sulfone Inhibitors for Repurposing Antibiotic Efficiency in Priority Pathogens》, the research content is summarized as follows. The ability of 6-(aryl)methylidene penicillin-based sulfones 1-7 to repurpose β-lactam antibiotics activity with bacterial species that carry carbapenem-hydrolyzing class D β-lactamases (OXA-23, OXA-24/40 and OXA-48), as well as with class A (TEM-1, CTX-M-2) and class C (CMY-2, DHA-1) enzymes, is reported. The combinations imipenem/3 and imipenem/4 restored almost completely the antibiotic efficacy in OXA-23 and OXA-24/40 carbapenemase-producing A. baumannii strains (1μg mL^-1) and also provided good results for OXA-48 carbapenemase-producing K. pneumoniae strains (4μg mL^-1). Compounds 2-6 in combinations with ceftazidime and ampicillin were also efficient in restoring antibiotic efficacy in E. coli strains carrying class C (CMY-2 and DHA-1) and class A (TEM-1 and CTX-M-2) β-lactamase enzymes, resp. Kinetic and inhibition studies with the OXA-24/40 enzyme, protein mass spectrometry anal. and docking studies allowed us to gain an insight into the inhibition mechanism and the exptl. observed differences between the ligands.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Product Details of C10H17BN2O2

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. SDS of cas: 761446-44-0.

Remya, Chandran;Dileep, K. V.;Koti Reddy, Eeda;Mantosh, Kumar;Lakshmi, Kesavan;Sarah Jacob, Reena;Sajith, Ayyiliyath M.;Jayadevi Variyar, E.;Anwar, Shaik;Zhang, Kam Y. J.;Sadasivan, C.;Omkumar, R. V. research published 《 Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase – Design, synthesis and biological evaluation》, the research content is summarized as follows. An novel high affinity multi-target directed ligands (MTDLs) against AChE and NMDAR, with reduced hepatotoxicity, performed in-silico structure-based modifications on tacrine, chem. synthesis of the derivatives and in-vitro validation of their activities. Nineteen such derivatives I [R = H, methylcarbamoyl, hydrazinecarbonyl, ethoxycarbonyl; R¹ = 2-furanyl, 1-methylpyrazol-4-yl, 2-FC₆H₄, etc.] showed inhibition with IC₅₀ values in the range of 18.53 ± 2.09 – 184.09 ± 19.23 nM against AChE and 0.27 ± 0.05 – 38.84 ± 9.64μM against NMDAR. Some of the selected compounds protected rat primary cortical neurons from glutamate induced excitotoxicity. Two of the tacrine derived MTDLs, I [R = H, R¹ = 1-methylpyrazol-4-yl; R = H, R¹ = 2-FC₆H₄] exhibited in-vivo efficacy in rats by protecting against behavioral impairment induced by administration of the excitotoxic agent, monosodium glutamate. Addnl., several of these synthesized compounds also exhibited promising inhibitory activitiy against butyrylcholinesterase. MTDL-201 I [R = H, R¹ = 1-methylpyrazol-4-yl] was also devoid of hepatotoxicity in-vivo. Given the therapeutic potential of MTDLs in disease-modifying therapy, studies revealed several promising MTDLs among which I [R = H, R¹ = 1-methylpyrazol-4-yl] appeared to be a potential candidate for immediate preclin. evaluations.

SDS of cas: 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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.

Ran, Kai;Zeng, Jun;Wan, Guoquan;He, Xiaojie;Feng, Zhanzhan;Xiang, Wang;Wei, Wei;Hu, Xiang;Wang, Ningyu;Liu, Zhihao;Yu, Luoting research published 《 Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors》, the research content is summarized as follows. Herein, the design and synthesis of pyrido[1,2-a]pyrimidinone derivatives I (R¹ = methoxyethoxy, tert-butoxycarbonyl-1,2,3,6-tetrahydropyridin-4-yl, 1H-pyrazol-4-yl, etc.) and II (R² = Me, azetidin-3-yl, etc.; R³ = 3-[(propan-2-yl)amino]propyl, prop-2-yn-1-yl, cyclopropylmethyl, etc.) as potent FGFR inhibitors were described. Examination of structure-activity relationships and preliminary assessment identified I (R¹ = 1-methyl-1H-pyrazol-4-yl) as a novel FGFR inhibitor that displayed excellent potency in vitro. Candidate I [R¹ = 1-methyl-1H-pyrazol-4-yl (III)] suppressed the phosphorylation of FGFR signaling pathways and induced cell cycle arrest and apoptosis at low nanomolar concentration In the kinase inhibition profile, III showed excellent kinase selectivity for the FGFR family. Furthermore, III showed higher aqueous solubility than Erdafitinib. Moreover, III exhibited potent antitumor activity (tumor growth inhibition = 106.4%) in FGFR2-amplified SNU-16 gastric cancer xenograft model using a daily oral dose of 30 mg/kg. These results suggest that III is a promising candidate for further drug development.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Category: pyrazoles-derivatives

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. HPLC of Formula: 761446-44-0.

Pei, Haixiang;Qin, Juliang;Wang, Fengmian;Tan, Binghe;Zhao, Zeda;Peng, Yangrui;Yu, Fangfei;Li, Ennian;Liu, Mingyao;Zhang, Rong;Liu, Bo;Du, Bing;Chen, Yihua research published 《 Discovery of potent ureido tetrahydrocarbazole derivatives for cancer treatments through targeting tumor-associated macrophages》, the research content is summarized as follows. For discovering novel compounds that target Tumor-associated macrophages (TAM), a series of ureido tetrahydrocarbazole derivatives I (R = 5-cyclopropylaminocarbonyl, 6-(morpholine-4-carbonyl), 7-isopropylaminocarbonyl, 8-(1-methylpiperazine-4-carbonyl), etc.) was designed, synthesized and evaluated both in vitro and in vivo. Among them, compound I (R = 5-(1-methyl-1H-pyrazole-4-yl)) was found to dose-dependently repolarize TAMs from M2 to M1 both in vitro and in vivo. And more importantly, the in vivo experiments also revealed that compound I (R = 5-(1-methyl-1H-pyrazole-4-yl)) was capable of remarkably inhibiting tumor growth of the LLC mouse model. Moreover, the synergy of compound I (R = 5-(1-methyl-1H-pyrazole-4-yl)) with anti-PD-1 antibody had more superior antineoplastic effects than the exclusive use of either in vivo.

HPLC of Formula: 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Application of C10H17BN2O2.

Nemec, Vaclav;Hylsova, Michaela;Maier, Lukas;Flegel, Jana;Sievers, Sonja;Ziegler, Slava;Schroeder, Martin;Berger, Benedict-Tilman;Chaikuad, Apirat;Valcikova, Barbora;Uldrijan, Stjepan;Drapela, Stanislav;Soucek, Karel;Waldmann, Herbert;Knapp, Stefan;Paruch, Kamil research published 《 Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway》, the research content is summarized as follows. Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines, e.g. I, afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines, e.g. II, revealed sub-micromolar modulators of the Hedgehog pathway.

Application of C10H17BN2O2, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Electric Literature of 761446-44-0.

Ng, Pearly Shuyi;Foo, Klement;Sim, Sandra;Wang, Gang;Huang, Chuhui;Tan, Li Hong;Poulsen, Anders;Liu, Boping;Tee, Doris Hui Ying;Ahmad, Nur Huda Binte;Wang, Sifang;Ke, Zhiyuan;Lee, May Ann;Kwek, Zekui P.;Joy, Joma;Anantharajan, Jothi;Baburajendran, Nithya;Pendharkar, Vishal;Manoharan, Vithya;Vuddagiri, Susmitha;Sangthongpitag, Kanda;Hill, Jeffrey;Keller, Thomas H.;Hung, Alvin W. research published 《 Fragment-based lead discovery of indazole-based compounds as AXL kinase inhibitors》, the research content is summarized as follows. AXL is a member of the TAM (TYRO3, AXL, MER) subfamily of receptor tyrosine kinases. It is upregulated in a variety of cancers and its overexpression is associated with poor disease prognosis and acquired drug resistance. Utilizing a fragment-based lead discovery approach, a new indazole-based AXL inhibitor was obtained. The indazole fragment hit 11, identified through a high concentration biochem. screen, was expeditiously improved to fragment 24 by screening our inhouse expanded library of fragments (ELF) collection. Subsequent fragment optimization guided by docking studies provided potent inhibitor 54 with moderate exposure levels in mice. X-ray crystal structure of analog 50 complexed with the I650M mutated kinase domain of Mer revealed the key binding interactions for the scaffold. The good potency coupled with reasonable kinase selectivity, moderate in vivo exposure levels, and availability of structural information for the series makes it a suitable starting point for further optimization efforts.

Electric Literature of 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Product Details of C10H17BN2O2.

Nemec, Vaclav;Maier, Lukas;Berger, Benedict-Tilman;Chaikuad, Apirat;Drapela, Stanislav;Soucek, Karel;Knapp, Stefan;Paruch, Kamil research published 《 Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core》, the research content is summarized as follows. The furo [3,2-b]pyridine motif represents a relatively underexplored central pharmacophore in the area of kinase inhibitors. Herein, author’s report flexible synthesis of 3,5-disubstituted furo[3,2-b]pyridines that relies on chemoselective couplings of newly prepared 5-chloro-3-iodofuro[3,2-b]pyridine. This methodol. allowed efficient second-generation synthesis of the state-of-the-art chem. biol. probe for CLK1/2/4 I, and identification of the highly selective inhibitors of HIPKs II and III which are presented and characterized in this study, including the X-ray crystal structure of II in HIPK2.chem. biol. probe.

Product Details of C10H17BN2O2, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Miwa, Shohei;Yokota, Masahiro;Ueyama, Yoshifumi;Maeda, Katsuya;Ogoshi, Yosuke;Seki, Noriyoshi;Ogawa, Naoki;Nishihata, Jun;Nomura, Akihiro;Adachi, Tsuyoshi;Kitao, Yuki;Nozawa, Keisuke;Ishikawa, Tomohiro;Ukaji, Yutaka;Shiozaki, Makoto research published 《 Discovery of Selective Transforming Growth Factor β Type II Receptor Inhibitors as Antifibrosis Agents》, the research content is summarized as follows. Historically, modulation of transforming growth factor β (TGF-β) signaling has been deemed a rational strategy to treat many disorders, though few successful examples have been reported to date. This difficulty could be partially attributed to the challenges of achieving good specificity over many closely related enzymes that are implicated in distinct phenotypes in organ development and in tissue homeostasis. Recently, fresolimumab and disitertide, two peptidic TGF-β blockers, demonstrated significant therapeutic effects toward human skin fibrosis. Therefore, the selective blockage of TGF-β signaling assures a viable treatment option for fibrotic skin disorders such as systemic sclerosis (SSc). In this report, we disclose selective TGF-β type II receptor (TGF-βRII) inhibitors that exhibited high functional selectivity in cell-based assays. The representative compound 29 attenuated collagen type I alpha 1 chain (COL1A1) expression in a mouse fibrosis model, which suggests that selective inhibition of TGF-βRII-dependent signaling could be a new treatment for fibrotic disorders.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Recommanded Product: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Related Products of 761446-44-0.

Miller, Susanne L.;Chotana, Ghayoor A.;Fritz, Jonathan A.;Chattopadhyay, Buddhadeb;Maleczka, Robert E. Jr.;Smith, Milton R. III research published 《 C-H Borylation Catalysts that Distinguish Between Similarly Sized Substituents Like Fluorine and Hydrogen》, the research content is summarized as follows. By modifying ligand steric and electronic profiles it is possible to C-H borylate ortho or meta to substituents in aromatic and heteroaromatic compounds, where steric differences between accessible C-H sites are small. Dramatic effects on selectivities between reactions using B₂pin₂ or 4,4,5,5-tetramethyl-1,3,2-dioxaborolane (HBpin) are described for the 1st time. Judicious ligand and borane combinations give highly regioselective C-H borylations on substrates where typical borylation protocols afford poor selectivities.

Related Products of 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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. Electric Literature of 761446-44-0.

Miles, Dillon H.;Yan, Xuelei;Thomas-Tran, Rhiannon;Fournier, Jeremy;Sharif, Ehesan U.;Drew, Samuel L.;Mata, Guillaume;Lawson, Kenneth V.;Ginn, Elaine;Wong, Kent;Soni, Divyank;Dhanota, Puja;Shaqfeh, Stefan G.;Meleza, Cesar;Chen, Ada;Pham, Amber T.;Park, Timothy;Swinarski, Debbie;Banuelos, Jesus;Schindler, Ulrike;Walters, Matthew J.;Walker, Nigel P.;Zhao, Xiaoning;Young, Stephen W.;Chen, Jie;Jin, Lixia;Leleti, Manmohan Reddy;Powers, Jay P.;Jeffrey, Jenna L. research published 《 Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors》, the research content is summarized as follows. The successful application of immunotherapy in the treatment of cancer relies on effective engagement of immune cells in the tumor microenvironment. Phosphoinositide 3-kinase γ (PI3Kγ) is highly expressed in tumor-associated macrophages, and its expression levels are associated with tumor immunosuppression and growth. Selective inhibition of PI3Kγ offers a promising strategy in immuno-oncol., which has led to the development of numerous potent PI3Kγ inhibitors with variable selectivity profiles. To facilitate further investigation of the therapeutic potential of PI3Kγ inhibition, we required a potent and PI3Kγ-selective tool compound with sufficient metabolic stability for use in future in vivo studies. Herein, we describe some of our efforts to realize this goal through the systematic study of SARs within a series of 7-azaindole-based PI3Kγ inhibitors. The large volume of data generated from this study helped guide our subsequent lead optimization efforts and will inform further development of PI3Kγ-selective inhibitors for use in immunomodulation.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Electric Literature of 761446-44-0

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