Day: November 21, 2022

Naik, R. D. published the artcileSynthesis of azo dyes using 2-amino-4,4′-dichlorodiphenyl ether 2′-sulfonic acid and their application on wool, nylon and silk as acid dyes, SDS of cas: 14580-22-4, the publication is Oriental Journal of Chemistry (1997), 13(3), 313-314, database is CAplus.

2-Amino-4,4′-dichloro-2′-sulfodiphenyl ether was diazotized and coupled with pyrazolone derivatives, γ Acid, or H Acid to give azo dyes that were used to dye wool, nylon, and silk. The fastness of the dyes to light and washing was tested.

Oriental Journal of 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 C10H9ClN2O, SDS of cas: 14580-22-4.

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

Mehta, K. H. published the artcileSynthesis of new heterocyclic thiazolidinone and azetidinone compounds and their antibacterial activity, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Asian Journal of Chemistry (2003), 15(1), 459-465, database is CAplus.

Thiazolidinones and azetidinones have been prepared by the reaction of various Schiff bases with thioglycolic acid and chloroacetyl chloride resp. The target compounds included methylenebis(4,1-phenylene)bis[9-thia-1,2,6-triazaspiro[4.4]non-2-en-7-one] derivatives I (R = Me, CO₂H; R¹ = H, Cl; R² = H, Cl, SO₃H; R³ = H, SO₃H; R⁴ = H, Cl, SO₃H) and methylenebis(4,1-phenylene)bis[1,5,6-triazaspiro[3.4]oct-6-en-2-one] derivatives II (R = Me, CO₂H; R¹ = H, Cl; R² = H, Cl, SO₃H; R³ = H, SO₃H; R⁴ = H, Cl, SO₃H). The structures of the compounds have been confirmed by elemental anal. and spectral anal. The antibacterial activity of the compounds has also been screened.

Asian Journal of 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 C10H9ClN2O, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Desai, C. K. published the artcileSynthesis of azo dyes using 4-amino-2,4′-dichlorodiphenyl ether and their application on wool, nylon and silk fibres, Category: pyrazoles-derivatives, the publication is Oriental Journal of Chemistry (1999), 15(2), 381-382, database is CAplus.

New azo acid dyes using 4-amino-2,4′-dichlorodiphenyl ether as the diazo component and pyrazolones as the coupling components were synthesized. The dyes were characterized by elemental anal. and IR spectra. The dyeing properties on various textile fabrics were investigated. The dyes were water soluble and applied at 90-100°C on cotton, silk, nylon, and wool.

Oriental Journal of 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 C10H9ClN2O, Category: pyrazoles-derivatives.

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

Bhavsar, R. A. published the artcileSynthesis of some trisazo pyrazolone acid dyes and their application on wool and nylon, Computed Properties of 14580-22-4, the publication is Asian Journal of Chemistry (1998), 10(4), 1061-1062, database is CAplus.

Monoazo pyrazolone dyes are very common but trisazo pyrazolone dyes with an arylazo group in position-4 and a second arylazo group at position-4 of the Ph nucleus and a third arylazo group at position-7 of the naphthyl nucleus of H- or γ-acid are not available. In the preparation of the title dyes, an aryldiazonium chloride is coupled in alk. medium with 1-phenyl-3-methyl-5-pyrazolone or 1-(2-chlorophenyl)-3-methyl-5-pyrazolone and the second arylazo group in position-4 of the 1-Ph group is introduced in acidic medium and the third arylazo group in position-7 of the 4-naphthyl group of H- or γ-acid is applied in alk. medium. Light fastness on wool was 4-5 to 5-6 and 3-4 to 5-6 on polyamide. Wash fastness was 3-4 to 4-5 on wool and 2-3 to 3-4 on polyamide.

Asian Journal of 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 C10H9ClN2O, Computed Properties of 14580-22-4.

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

Mehta, K. H. published the artcileSynthesis of new heterocyclic pyrazoline and isoxazoline compounds and their antibacterial activity, SDS of cas: 14580-22-4, the publication is Chemistry: An Indian Journal (2003), 1(1), 38-41, database is CAplus.

1-(2-Chlorophenyl)-3-methyl-5-pyrazolone was condensed with different aromatic aldehydes RC₆H₄CHO (R = 2-MeO, 3-NO₂, 3-OH-4-MeO, etc.) to yield arylidine derivatives I in 61-72% yield. I were further reacted with phenylhydrazine or hydroxylamine hydrochloride to yield 3-methyl-1,4,5-triphenylpyrazolo[3,4-c]pyrazole II (X = N-Ph) (63-70%) and 4-methyl-3,6-diphenylpyrazolo[3,4-c]isoxazole II (X = O) (62-72%) derivatives, resp. The prepared compounds showed antibacterial activity against S. aureus E. coli.

Chemistry: An Indian Journal 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, SDS of cas: 14580-22-4.

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

Kaiser, Thomas M. published the artcileProspective evaluation and success of a machine learning hit-to-lead drug development program against phosphatidylinositol 3-kinase α, SDS of cas: 1416437-27-8, the publication is ARKIVOC (Gainesville, FL, United States) (2021), 25-43, database is CAplus.

A cheminformatics protocol which dramatically increases quality candidate identification and should reduce attrition rate of compounds entering clinic, increasing cost-effectiveness of drug development is described. All N-(5-(3-aryl)(imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)benzenesulfonamides I [Ar = pyrimidin-2-yl, pyrazolo[1,5-a]pyrimidin-6-yl, 2-(dimethylamino)pyrimidin-5-yl, 5-ethyl-1,2,4-oxadiazol-3-yl, 2-methoxypyrimidin-5-yl] synthesized from protocol were found to have low nanomolar activity against oncol. target phosphatidylinositol 3-kinase α. Therefore it was proposed that this protocol could be used as a tool for reducing synthetic burden required for hit-to-lead optimization.

ARKIVOC (Gainesville, FL, United States) published new progress about 1416437-27-8. 1416437-27-8 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronate Esters,Boronic acid and ester, name is 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyrimidine, and the molecular formula is C12H16BN3O2, SDS of cas: 1416437-27-8.

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

Desroy, Nicolas published the artcileNovel HldE-K Inhibitors Leading to Attenuated Gram Negative Bacterial Virulence, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2013), 56(4), 1418-1430, database is CAplus and MEDLINE.

The optimization of an HldE kinase inhibitor to low nanomolar potency is reported here, which resulted in the identification of the first reported compounds active on selected Escherichia coli strains. One of the most interesting candidates, compound 86, was shown to inhibit specifically bacterial LPS heptosylation on efflux pump deleted E. coli strains. This compound did not interfere with E. coli bacterial growth (MIC > 32 μg/mL) but sensitized this pathogen to hydrophobic antibiotics like macrolides normally inactive on Gram-neg. bacteria. In addition, 86 could sensitize E. coli to serum complement killing. These results demonstrate that HldE kinase is a suitable target for drug discovery. They also pave the way toward novel possibilities of treating or preventing bloodstream infections caused by pathogenic Gram-neg. bacteria by inhibiting specific virulence factors.

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, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.

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

Sijm, Maarten published the artcileIdentification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors, Computed Properties of 763120-58-7, the publication is ChemMedChem (2020), 15(2), 219-227, database is CAplus and MEDLINE.

Leishmaniasis is a neglected parasitic disease caused by over 20 different Leishmania species. Current treatments often rely on harsh regimes of pentavalent antimonials such as sodium stibogluconate, while more recent drugs suffer other shortcomings such as low stability and rapid emergence of treatment failure, amongst others. Furthermore, the effectiveness of drugs varies depending on the infecting Leishmania species, thus there is an urgent need for new and effective anti-leishmanial drugs. Screening of an inhouse compound library identified the hexahydrophthalazinone NPD-2942 as a low micromolar hit with a pIC₅₀ of 5.8 against L. infantum and a pIC₅₀ of 4.6 for cytotoxicity against human MRC-5 fibroblasts. To derive structure-activity relationships, we modified the cyclohexyl ring of the hexahydrophthalazinone scaffold and 1,2,3-triazoles were attempted as replacement for the pyrazole ring, amongst others. Ultimately, the 2,3-pyrazole-substituted hexahydrophthalazinone NPD-1289 was identified as the most potent analog in this series with a pIC₅₀ of 6.3, although some cytotoxicity toward MRC-5 cells (pIC₅₀=5.1) was recorded as well. Replacement of the unsubstituted 2,3-pyrazole with 1,2,3-triazoles led to compounds with lower anti-leishmanial activity. The current scaffold is a valuable new starting point for optimization toward novel anti-leishmanial drugs.

ChemMedChem 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 C10H13NO2, Computed Properties of 763120-58-7.

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

Kwak, Se Hun published the artcileN-Aminopyridinium Ylide-Directed, Copper-Promoted Amination of sp² C-H Bonds, HPLC of Formula: 930-36-9, the publication is Journal of Organic Chemistry (2019), 84(20), 13022-13032, database is CAplus and MEDLINE.

N-Aminopyridinium ylides were used as monodentate directing groups for copper-promoted C-H/N-H coupling of sp² C-H bonds with pyrazoles, imidazoles, and sulfonamides. Reactions proceed in fluorinated alc. solvents at elevated temperatures and require use of 1.3-3 equiv of copper(II) acetate. This appears to be the first method for copper-promoted C-H/N-H coupling directed by a removable monodentate auxiliary in absence of added ligands.

Journal of Organic Chemistry 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, HPLC of Formula: 930-36-9.

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

Duffy, Kevin J. published the artcileHydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis, Quality Control of 14580-22-4, the publication is Journal of Medicinal Chemistry (2001), 44(22), 3730-3745, database is CAplus and MEDLINE.

High-throughput screening for the induction of a luciferase reporter gene in a thrombopoietin (TPO)-responsive cell line resulted in the identification of 4-diazo-3-hydroxy-1-naphthalenesulfonic acids as TPO mimics. Modification of the core structure and adjustment of unwanted functionality resulted in the development of (5-oxo-1,5-dihydropyrazol-4-ylidene)hydrazines which exhibited efficacies equivalent to those of TPO in several cell-based assays designed to measure thrombopoietic activity. Furthermore, these compounds elicited biochem. responses in TPO-receptor-expressing cells similar to those in TPO itself, including kinase activation and protein phosphorylation. Potencies for the best compounds were high for such low mol. weight compounds (MW < 500) with EC₅₀ values in the region of 1-20 nM.

Journal of Medicinal 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 C10H9ClN2O, Quality Control of 14580-22-4.

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