Day: November 21, 2022

Meredith, Erik L. published the artcileIdentification of Potent and Selective Amidobipyridyl Inhibitors of Protein Kinase D, Safety of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(15), 5422-5438, database is CAplus and MEDLINE.

The synthesis and biol. evaluation of potent and selective PKD (protein kinase D) inhibitors, e.g. I, are described herein. The compounds described in the present study selectively inhibit PKD among other putative HDAC (Histone deacetylase) kinases. The PKD inhibitors of the present study blunt phosphorylation and subsequent nuclear export of HDAC4/5 in response to diverse agonists. These compounds further establish the central role of PKD as an HDAC4/5 kinase and enhance the current understanding of cardiac myocyte signal transduction. The in vivo efficacy of a representative example compound on heart morphol. is reported herein.

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, Safety of 1H-Pyrazole-4-boronic acid.

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

Meredith, Erik L. published the artcileIdentification of Potent and Selective Amidobipyridyl Inhibitors of Protein Kinase D, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(15), 5422-5438, database is CAplus and MEDLINE.

The synthesis and biol. evaluation of potent and selective PKD (protein kinase D) inhibitors, e.g. I, are described herein. The compounds described in the present study selectively inhibit PKD among other putative HDAC (Histone deacetylase) kinases. The PKD inhibitors of the present study blunt phosphorylation and subsequent nuclear export of HDAC4/5 in response to diverse agonists. These compounds further establish the central role of PKD as an HDAC4/5 kinase and enhance the current understanding of cardiac myocyte signal transduction. The in vivo efficacy of a representative example compound on heart morphol. is reported herein.

Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Name: (1H-Pyrazol-5-yl)boronic acid.

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

Monastyrskyi, Andrii published the artcileDiscovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors, Formula: C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(3), 400-404, database is CAplus and MEDLINE.

The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, the authors used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 (N-(3-(quinazolin-2-ylamino)phenyl)acetamide) and 23 (N-(3-(6-((N-pyrazol-4-yl)quinazolin-2-yl)amino)phenyl)acetamide), with submicromolar inhibitory activities against ASK1. Kinetic anal. demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described herein are ATP competitive.

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, Formula: C3H5BN2O2.

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

Amiri, Zeinab published the artcileA catalyst-free approach to synthesis of spiroacenaphthylene-pyranopyrazole derivatives in water media, HPLC of Formula: 14580-22-4, the publication is Molecular Diversity (2021), 25(1), 121-129, database is CAplus and MEDLINE.

A simple approach for the synthesis of spiroacenaphthylene-pyranopyrazole derivatives was achieved via the reaction between acenaphthoquinone, pyrazolones, and activated methylene compounds (malononitrile derivatives) in water as a green solvent without using any catalyst in order to avoid the use of transition metal. This method has the advantages of mild reaction condition, short reaction time, easy workup, excellent yields, and avoidance of environmentally hazardous solvents.

Molecular Diversity published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, HPLC of Formula: 14580-22-4.

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

Kudashev, Anton published the artcileSite-Selective Pd-Catalyzed C(sp³)-H Arylation of Heteroaromatic Ketones, Recommanded Product: 1-Methylpyrazole, the publication is Chemistry – A European Journal (2021), 27(70), 17688-17694, database is CAplus and MEDLINE.

A ligand-controlled site-selective C(sp³)-H arylation of heteroaromatic ketones had been developed using Pd catalysis to gave ArC(O)CHR¹CH₂R² [Ar = thiazol-2-yl, 2-pyridyl, 2-quinolyl, etc.; R¹ = Ph, 4-MeC₆H₄, 2-naphthyl, etc.; R² = H, Me, ph, etc.]. The reaction occurred selectively at the α- or β-position of the ketone side-chain. The switch from α- or β-arylation was realized by addition of a pyridone ligand. The α-arylation process showed broad scope and high site- and chemoselectivity, whereas the β-arylation was more limited. Mechanistic investigations suggested that α-arylation occurs through C-H activation/oxidative addition/reductive elimination whereas β-arylation involves desaturation and aryl insertion.

Chemistry – A European Journal published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Recommanded Product: 1-Methylpyrazole.

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

Sabate-Alduy, Catherine published the artcile1,3-Dipolar cycloaddition of diazomethane Orientation of the addition of diazoalkanes to acetylenic compounds α-substituted with an alcohol or an ether group, Product Details of C5H8N2O, the publication is Bulletin de la Societe Chimique de France (1972), 2764-9, database is CAplus.

The reaction of CH2N2 with acetylenic alcs. RR1CR2CCH (R and R1 = H, Me, Ph; (RR1) = (CH2)5; R2 = OH, NH2, OMe) was not stereospecific, giving 40-80% of the pyrazoles I and 20-60% of their isomers II (R3 = H). On the other hand the reaction with MeCHN2 was stereospecific, giving 80-100% I (R3 = Me). CH2N2 reacted with Me 3-(1-hydroxycyclohexyl)-propiolate to give 100% II [(RR1) = (CH2)5, R2 = OH, R3 = CO2Me , whereas with MeCHN2 a mixture of the isomers was obtained. Charge distribution calculations by the CNDO/2 method confirm that the polarity of the acetylenic mol. determines the direction of the addition, rather than steric effects.

Bulletin de la Societe Chimique de France published new progress about 37599-34-1. 37599-34-1 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Ether, name is 4-(methoxymethyl)-1H-pyrazole, and the molecular formula is C5H8N2O, Product Details of C5H8N2O.

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

Favalli, Nicholas published the artcileLarge screening of DNA-compatible reaction conditions for Suzuki and Sonogashira cross-coupling reactions and for reverse amide bond formation, HPLC of Formula: 763120-58-7, the publication is Bioorganic & Medicinal Chemistry (2021), 116206, database is CAplus and MEDLINE.

Progress in DNA-encoded chem. library synthesis and screening crucially relies on the availability of DNA-compatible reactions, which proceed with high yields and excellent purity for a large number of possible building blocks. In the past, exptl. conditions have been presented for the execution of Suzuki and Sonogashira cross-coupling reactions on-DNA. In this article, our aim was to optimize Suzuki and Sonogashira reactions, comparing our results to previously published procedures. We have tested the performance of improved conditions using 606 building blocks (including boronic acids, pinacol boranes and terminal alkynes), achieving >70% conversion for 84% of the tested mols. Moreover, we describe efficient exptl. conditions for the on-DNA synthesis of amide bonds, starting from DNA derivatives carrying a carboxylic acid moiety and 300 primary, secondary and aromatic amines, as amide bonds are frequently found in DNA-encoded chem. libraries thanks to their excellent DNA compatibility.

Bioorganic & 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, HPLC of Formula: 763120-58-7.

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

Favalli, Nicholas published the artcileLarge screening of DNA-compatible reaction conditions for Suzuki and Sonogashira cross-coupling reactions and for reverse amide bond formation, Quality Control of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry (2021), 116206, database is CAplus and MEDLINE.

Progress in DNA-encoded chem. library synthesis and screening crucially relies on the availability of DNA-compatible reactions, which proceed with high yields and excellent purity for a large number of possible building blocks. In the past, exptl. conditions have been presented for the execution of Suzuki and Sonogashira cross-coupling reactions on-DNA. In this article, our aim was to optimize Suzuki and Sonogashira reactions, comparing our results to previously published procedures. We have tested the performance of improved conditions using 606 building blocks (including boronic acids, pinacol boranes and terminal alkynes), achieving >70% conversion for 84% of the tested mols. Moreover, we describe efficient exptl. conditions for the on-DNA synthesis of amide bonds, starting from DNA derivatives carrying a carboxylic acid moiety and 300 primary, secondary and aromatic amines, as amide bonds are frequently found in DNA-encoded chem. libraries thanks to their excellent DNA compatibility.

Bioorganic & Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Quality Control of 724710-02-5.

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

Thaker, B. T. published the artcileMicrowave assisted synthesis and characterization of unsymmetrical tetradentate Schiff base complexes of VO(IV) and MoO(V), Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy (2011), 84(1), 51-61, database is CAplus and MEDLINE.

Microwave synthesis, is green chem. method, simple, sensitive, reducing solvent amount and reaction time. The attempt was made to synthesize the unsym. tetradentate N₂O₂ ligands and their VO(IV) and MoO(V) unsym. tetradentate Schiff base complexes by classical and microwave techniques using domestic microwave oven. The resulting unsym. Schiff base ligands (I, X = H, 2-Cl, 3-SO₂NH₂, L¹-L³, resp.) were characterized by different spectral methods. Their complexes with oxocations of VO(IV) and MoO(V) were synthesized and characterized by elemental analyses, conductometric measurements, IR and electronic absorption, ¹H NMR spectra, mass spectrometry, ESR spectra, magnetic susceptibility measurement and thermal study. Probably the oxo metal ion is bonded to the ligand through the oxygen and imino nitrogen and the geometry around metal ion is distorted octahedral.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C6H12O2, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Thaker, B. T. published the artcileSynthesis, spectral, and thermal studies of oxomolybdenum(V) Schiff-base complexes derived from heterocyclic β-diketone, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Journal of Coordination Chemistry (2010), 63(9), 1597-1610, database is CAplus.

Six mononuclear Mo(V) Schiff-base complexes were prepared by the reaction of MoCl₅ with Schiff bases, namely HL¹-HL³ and HL⁴-HL⁶, formed from the reaction of 3-methyl-1-(2-chloro)phenyl-1H-pyrazol-5-one-4-carbaldehyde (I), 3-methyl-1-(3-chloro)phenyl-1H-pyrazol-5-one-4-carbaldehyde (II), and 3-methyl-1-(3-sulfonamido)phenyl-1H-pyrazol-5-one-4-carbaldehyde (III) with ethanolamine and propanolamine, resp., in aqueous ethanolic medium. The resulting complexes were characterized by elemental analyses, molar conductance, FTIR, ¹H NMR, electronic, ESR spectra, magnetic susceptibility, and thermal study. The molar conductivity data show them to be non-electrolytes. IR and ¹H NMR spectral data suggest that the ligand is a dibasic bidentate with ON donor toward metal ion. Electronic, magnetic, and ESR spectral data suggest that the oxomolybdenum(V) complexes have distorted octahedral geometry. One chloride coordinated to molybdenum is confirmed by thermal study.

Journal of Coordination Chemistry published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C4H7BN2O2, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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