Day: November 30, 2022

Asegbeloyin, J. N. published the artcileSynthesis, characterization and antimicrobial screening of some 4-acylpyrazoloimines and some 3d transition metal(II) complexes, Quality Control of 4551-69-3, the publication is Asian Journal of Chemistry (2014), 26(9), 2753-2758, database is CAplus.

Some acylhydroxypyrazole acylhydrazones, e.g., I (R = pentyl, Pr), and their 3d transition metal(II) complexes were synthesized. The ligands and their 3d transition metal complexes were characterized by elemental anal., molar conductance, magnetic susceptibility measurements and spectroscopic methods. The ligands behaved as mono-anion ONO or ONS donor mols. Microanal., electronic spectral and magnetic measurements showed the metal complexes as ML₂ type. All the synthesized compounds were screened for their in vitro antimicrobial activity against some gram pos. and gram neg. clin. bacterial strains. Antimicrobial activity test results showed that the metallic derivatives are more active against the bacterial strains than the imines.

Asian Journal of Chemistry published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Quality Control of 4551-69-3.

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

Kurasawa, Osamu published the artcileIdentification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones, Quality Control of 1009071-34-4, the publication is Bioorganic & Medicinal Chemistry (2017), 25(7), 2133-2147, database is CAplus and MEDLINE.

Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective tumor-cell death in a p53-dependent manner, suggesting that Cdc7 is an attractive target for the treatment of cancers. In order to identify a new class of potent Cdc7 inhibitors, we generated a putative pharmacophore model based on in silico docking anal. of a known inhibitor with Cdc7 homol. model. The pharmacophore model provided a min. structural motif of Cdc7 inhibitor, by which preliminary medicinal chem. efforts identified a dihydrothieno[3,2-d]-pyrimidin-4(1H)-one scaffold having a heteroaromatic hinge-binding moiety. The structure-activity relationship (SAR) studies resulted in the discovery of new, potent, and selective Cdc7 inhibitors 14a, c, e. Furthermore, the high selectivity of 14c, e for Cdc7 over Rho-associated protein kinase 1 (ROCK1) is discussed by utilizing a docking study with Cdc7 and ROCK2 crystal structures.

Bioorganic & Medicinal Chemistry published new progress about 1009071-34-4. 1009071-34-4 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester, name is tert-Butyl 3-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-carboxylate, and the molecular formula is C15H25BN2O4, Quality Control of 1009071-34-4.

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

Kublicki, Marcin published the artcile1,4-Phenylenebis((1-methyl-1H-pyrazol-5-yl)borinic 8-oxyquinolinate) as a photoredox catalyst in the atom transfer radical addition of iodoperfluoroalkanes to alkenyl groups bearing organoboron compounds, Category: pyrazoles-derivatives, the publication is Tetrahedron Letters (2019), 60(29), 1918-1923, database is CAplus.

The key photocatalytic properties of a transition-metal-free heteroleptic complex I (1) derived from 1,4-phenyldiboronic acid were evaluated. This compound was utilized in the atom transfer radical addition of iodoperfluoroalkanes C_nF_2n+1I (n = 1-4) to a series of allylic arylboronate compounds CH₂:CHCH₂XAr[B] [X = bond, O, CH₂; Ar = phenylene, thiophenediyl; [B] = B(OH)₂, BF₃K] to give C-I activation products, [B]ArXCH₂CHICH₂C_nF_2n+1 (2–14). The products of these reactions retained the B-C bond, and Suzuki-Miyaura coupling of one product gave biphenyl derivatives The X-ray anal. of one of the obtained perfluoroalkylated boronic acids revealed the presence of open star-shaped channels.

Tetrahedron Letters 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, Category: pyrazoles-derivatives.

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

Hong, Fang-Tsao published the artcileSmall Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket, HPLC of Formula: 724710-02-5, the publication is Journal of Medicinal Chemistry (2014), 57(14), 5949-5964, database is CAplus and MEDLINE.

Structure-activity relationship investigations conducted at the 5-position of the N-pyridine ring of a series of N-arylsulfonyl-N’-2-pyridinyl-piperazines led to the identification of a novel bis-pyridinyl piperazine sulfonamide I that was a potent disruptor of the glucokinase-glucokinase regulatory protein (GK-GKRP) interaction. Anal. of the x-ray cocrystal of compound I bound to hGKRP revealed that the 3-pyridine ring moiety occupied a previously unexplored binding pocket within the protein. Key features of this new binding mode included forming favorable contacts with the top face of the Ala27-Val28-Pro29 (“shelf region”) as well as an edge-to-face interaction with the Tyr24 side chain. Compound I was potent in both biochem. and cellular assays (IC₅₀ = 0.005 μM and EC₅₀ = 0.205 μM, resp.) and exhibited acceptable pharmacokinetic properties for in vivo evaluation. When administered to db/db mice (100 mg/kg, po), compound I demonstrated a robust pharmacodynamic effect and significantly reduced blood glucose levels up to 6 h postdose.

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, HPLC of Formula: 724710-02-5.

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

Bercean, Vasile-Nicolae published the artcileAzo compounds derived from 1H-5-amino-4-ethoxycarbonyl-3-methyl-pyrazole and phenols or phenolic derivatives and possibilities of their cyclization to pyrazolo[5,1-c]benzo[1,2-e][1,2,4]triazines, Computed Properties of 23286-70-6, the publication is Revista de Chimie (Bucharest, Romania) (2011), 62(2), 154-157, database is CAplus.

The coupling reaction of 1H-4-ethoxycarbonyl-3-methylpyrazol-5-yldiazonium chloride with phenols and phenolic derivatives led to 1H-5-arylazo-4-ethoxycarbonyl-3-methylpyrazoles. Cyclization of one of the latter compounds, [1H-4-ethoxycarbonyl-5-(4,6-dimethoxy-2-hydroxyphenylazo)-3-methylpyrazole] gave the corresponding pyrazolo[5,1-c]benzo[1,2-e][1,2,4]triazine.

Revista de Chimie (Bucharest, Romania) published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C7H11N3O2, Computed Properties of 23286-70-6.

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

Bercean, Vasile-Nicolae published the artcileNew azo compounds derived from 1H-5-amino-4-ethoxycarbonyl-3-methyl-pyrazole and 3-mono- or 1,3-disubstituted pyrazol-5-ones, Synthetic Route of 23286-70-6, the publication is Revista de Chimie (Bucharest, Romania) (2010), 61(4), 364-367, database is CAplus.

Pyrazole-derived azo compounds were designed, and the synthesis of the target compounds was achieved by a coupling reaction of 3-amino-5-methyl-1H-pyrazole-4-carboxylic acid Et ester (I) with pyrazolone derivatives The products thus obtained were confirmed by MS, IR, UV-VIS, ¹H-NMR, and ¹³C-NMR, and existed in multiple tautomeric forms.

Revista de Chimie (Bucharest, Romania) published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C7H11N3O2, Synthetic Route of 23286-70-6.

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