Category: 763120-58-7

Duncton, Matthew A. J. published the artcileArylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(6), 1579-1581, database is CAplus and MEDLINE.

A novel class of 1-(isoquinolin-5-yl)-4-arylamino-phthalazines is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity with an IC₅₀ as low as 0.017 μM in an HTRF enzymic assay. The compounds also inhibit VEGFR-1, a related tyrosine kinase.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Kudo, Noriaki published the artcileA versatile method for Suzuki cross-coupling reactions of nitrogen heterocycles, Category: pyrazoles-derivatives, the publication is Angewandte Chemie, International Edition (2006), 45(8), 1282-1284, database is CAplus and MEDLINE.

A wide-ranging study of Suzuki reactions which use nitrogen-containing heterocycles was described. This method was highly versatile (a single procedure was used for all substrates, including boronate esters and trifluoroborates), compatible with a variety of unprotected functionalities (e.g., NH₂– and OH-substituted substrates), and efficient even with inactivated aryl chlorides.

Angewandte Chemie, International Edition published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Nie, Zhe published the artcileStructure-based design, synthesis, and study of potent inhibitors of β-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2005), 48(5), 1596-1609, database is CAplus and MEDLINE.

Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. FabH, β-ketoacyl-ACP synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-pos. and -neg. bacteria. Small mols. that inhibit FabH enzymic activity have the potential to be candidates within a class of selective, nontoxic, and broad-spectrum antibacterials. Using crystallog. structural information on these highly conserved active sites and structure based drug design principles, a benzoylaminobenzoic acid series of compounds was developed as potent inhibitors of FabH. This class of inhibitors, e.g., I, demonstrated strong antibacterial activity against Gram-pos. and selected Gram-neg. organisms.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Venier, Olivier published the artcilePyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1, Application of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(8), 2244-2251, database is CAplus and MEDLINE.

A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chem. optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C4H3Cl2N3, Application of 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Yang, Shu-Wei published the artcileBenzimidazole analogs as WTA biosynthesis inhibitors targeting methicillin resistant Staphylococcus aureus, Safety of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(19), 4743-4747, database is CAplus and MEDLINE.

A series of benzimidazole analogs have been synthesized to improve the profile of the previous lead compounds tarocin B. The syntheses, structure-activity relationships, and selected biochem. data of these analogs are described. The optimization efforts allowed the identification of I, a fluoro-substituted benzimidazole, exhibiting potent TarO inhibitory activity and typical profile for a wall teichoic acid (WTA) biosynthesis inhibitor. Compound I displayed a potent synergistic and bactericidal effect in combination with imipenem against diverse methicillin-resistant Staphylococci.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C5H7BO2S, Safety of 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Deng, Xianming published the artcileExpanding the Diversity of Allosteric Bcr-Abl Inhibitors, Category: pyrazoles-derivatives, the publication is Journal of Medicinal Chemistry (2010), 53(19), 6934-6946, database is CAplus and MEDLINE.

Inhibition of Bcr-Abl kinase activity by imatinib for the treatment of chronic myeloid leukemia (CML) currently serves as the paradigm for targeting dominant oncogenes with small mols. The discovery of GNF-2 (I, R = H) and GNF-5 (I, R = CH₂CH₂OH) was recently reported as selective non-ATP competitive inhibitors of cellular Bcr-Abl kinase activity that target the myristate binding site. Herein is used cell-based structure-activity relationships to guide the optimization and diversification of ligands that are capable of binding to the myristate binding site and rationalize the findings based upon an Abl-compound I (R = H) cocrystal. The structure-activity relationships required to obtain potent antiproliferative activity against Bcr-Abl transformed cells is elucidated, and the discovery of new compounds II (R¹ = 4-(NH₂SO₂)C₆H₄, 4-(MeSO₂NH)C₆H₄, 4-pyrazolyl), III, and IV that display improved potency or pharmacol. properties is reported. This work demonstrates that a variety of structures can effectively target the Bcr-Abl myristate binding site and provides new leads for developing drugs that can target this binding site.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Machrouhi, Fouzia published the artcileThe rational design of a novel potent analogue of the 5′-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity, SDS of cas: 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(22), 6394-6399, database is CAplus and MEDLINE.

We have designed and synthesized analogs of compound C, [4-(2-piperidinyl-1-ylethoxy)phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine, a non-specific inhibitor of 5′-AMP-activated protein kinase (AMPK), using a computational fragment-based drug design (FBDD) approach. Synthesizing only twenty-seven analogs yielded a compound that was equipotent to compound C in the inhibition of the human AMPK (hAMPK) α2 subunit in the heterotrimeric complex in vitro, exhibited significantly improved selectivity against a subset of relevant kinases, and demonstrated enhanced cellular inhibition of AMPK.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, SDS of cas: 763120-58-7.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Caroff, Eva published the artcileOptimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y₁₂ antagonists for inhibition of platelet aggregation, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(17), 4323-4331, database is CAplus and MEDLINE.

2-Phenyl-4-pyrimidinecarboxamide analogs were identified as P2Y₁₂ antagonists. Optimization of the carbon-linked or nitrogen-linked substituent at the 6-position of the pyrimidine ring provided compounds with excellent ex vivo potency in the platelet aggregation assay in human plasma. One compound met the objectives for activity, selectivity and ADMET properties. The synthesis of the target compounds was achieved using (γS)-γ-[[(6-chloro-2-phenyl-4-pyrimidinyl)carbonyl]amino]-4-(ethoxycarbonyl)-δ-oxo-1-piperazinepentanoic acid 1,1-dimethylethyl ester and (γS)-4-(butoxycarbonyl)-γ-[[(6-chloro-2-phenyl-4-pyrimidinyl)carbonyl]amino]-δ-oxo-1-piperazinepentanoic acid 1,1-dimethylethyl ester as key intermediates.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Caroff, Eva published the artcileOptimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y₁₂ antagonists for inhibition of platelet aggregation, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(17), 4323-4331, database is CAplus and MEDLINE.

2-Phenyl-4-pyrimidinecarboxamide analogs were identified as P2Y₁₂ antagonists. Optimization of the carbon-linked or nitrogen-linked substituent at the 6-position of the pyrimidine ring provided compounds with excellent ex vivo potency in the platelet aggregation assay in human plasma. One compound met the objectives for activity, selectivity and ADMET properties. The synthesis of the target compounds was achieved using (γS)-γ-[[(6-chloro-2-phenyl-4-pyrimidinyl)carbonyl]amino]-4-(ethoxycarbonyl)-δ-oxo-1-piperazinepentanoic acid 1,1-dimethylethyl ester and (γS)-4-(butoxycarbonyl)-γ-[[(6-chloro-2-phenyl-4-pyrimidinyl)carbonyl]amino]-δ-oxo-1-piperazinepentanoic acid 1,1-dimethylethyl ester as key intermediates.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Cox, Paul A. published the artcileProtodeboronation of Heteroaromatic, Vinyl, and Cyclopropyl Boronic Acids: pH-Rate Profiles, Autocatalysis, and Disproportionation, Quality Control of 763120-58-7, the publication is Journal of the American Chemical Society (2016), 138(29), 9145-9157, database is CAplus and MEDLINE.

PH-rate profiles for aqueous-organic protodeboronation of 18 boronic acids, many widely viewed as unstable, have been studied by NMR and DFT. Rates were pH-dependent, and varied substantially between the boronic acids, with rate maxima that varied over 6 orders of magnitude. A mechanistic model containing five general pathways (k₁-k₅) has been developed, and together with input of [B]_tot, K_W, K_a, and K_aH, the protodeboronation kinetics can be correlated as a function of pH (1-13) for all 18 species. Cyclopropyl and vinyl boronic acids undergo very slow protodeboronation, as do 3- and 4-pyridyl boronic acids (t_0.5 > 1 wk, pH 12, 70 °C). In contrast, 2-pyridyl and 5-thiazolyl boronic acids undergo rapid protodeboronation (t_0.5 ≈ 25-50 s, pH 7, 70 °C), via fragmentation of zwitterionic intermediates. Lewis acid additives (e.g., Cu, Zn salts) can attenuate (2-pyridyl) or accelerate (5-thiazolyl and 5-pyrazolyl) fragmentation. Two addnl. processes compete when the boronic acid and the boronate are present in sufficient proportions (pH = pK_a ± 1.6): (i) self-/autocatalysis and (ii) sequential disproportionations of boronic acid to borinic acid and borane.

Journal of the American Chemical Society published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Quality Control of 763120-58-7.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics