Category: pyrazoles-derivatives

Parekh, Nikhil M. published the artcileAntituberculosis and antibacterial evaluations of some novel phenyl pyrazolone-substituted 1H-benzo[g]pyrazolo[3,4-b]quinoline-3-ylamine derivatives, Product Details of C10H9ClN2O, the publication is Medicinal Chemistry Research (2012), 21(12), 4168-4176, database is CAplus.

Coupling of various phenylpyrazolone derivatives with diazonium salt of 1H-benzo[g]pyrazolo[3,4-b]quinolin-3-ylamine gave a series of heterocyclic azo compounds All the synthesized azo compounds have been characterized by their percentage yield, elemental, and spectral analyses. These new compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. Furthermore, the synthesized compounds were tested for in vitro antituberculosis activity against Mycobacterium tuberculosis. Streptomycin, Isoniazid, Rifampicin, and Ethambutol were used as standards in this investigation.

Medicinal Chemistry Research 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, Product Details of C10H9ClN2O.

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

Parekh, Nikhil M. published the artcileSynthesis of heterocyclic monoazo dyes derived from 1H-benzo[g]pyrazolo[3,4-b]quinoline-3-ylamine: their antimicrobial activity and their dyeing performance on various fibers, Application In Synthesis of 14580-22-4, the publication is Research on Chemical Intermediates (2012), 38(3-5), 885-901, database is CAplus.

Heterocyclic monoazobenzoquinoline-based azo dyes have been derived by diazotization of 1H-benzo[g]pyrazolo[3,4-b]quinoline-3-ylamine with a variety of phenylpyrazolone-based coupling compounds The synthesized dyes were characterized by determination of their percentage yield, by elemental anal., and by UV-visible, IR, and ¹H NMR spectroscopy. Dyeing performance on silk, wool, nylon, and polyester fibers was assessed. The fastness properties of the dyes on each fiber were moderate to excellent. The antimicrobial activity of the dyes at different concentrations were also examined, by use of the Kirby-Bauer disk diffusion method.

Research on Chemical Intermediates 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, Application In Synthesis of 14580-22-4.

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

Parekh, Nikhil M. published the artcileDyeing performance of heterocyclic monoazo dyes based on 3-amino-1H-pyrazolon[3,4-b]quinoline derivatives on various fibers, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Archives of Applied Science Research (2011), 3(4), 359-365, database is CAplus.

1H-Pyrazolo[3,4-b]quinolin-3-amine derivatives have been synthesized by the reaction between substituted Ph pyrazolones and 3-amino-1H-pyrazolon[3,4-b]quinoline. The novel compound structures have been established on the basis of their substituted Ph pyrazolones derivatives All the azo compounds were characterized by their percentage yield, m.p., elemental anal., UV visible spectra, IR spectra, NMR spectra and dyeing performance on nylon, wool, silk and polyester fibers. All the synthesized dyes gave moderate to excellent fastness properties on each fiber.

Archives of Applied Science Research 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, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Wipf, Peter published the artcileMetathesis reactions of pyrazolotriazinones generate dynamic combinatorial libraries, Product Details of C7H10N2O2, the publication is Organic Letters (2005), 7(20), 4483-4486, database is CAplus and MEDLINE.

Reversible metathesis reactions of pyrazolotriazinones and aliphatic aldehydes or ketones proceed in aqueous, phosphate-buffered media at pH 4 and 40-60 °C to generate thermodynamically controlled mixtures of heterocycles.

Organic Letters published new progress about 890590-91-7. 890590-91-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid, name is 3-Isopropyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C3H6O2, Product Details of C7H10N2O2.

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

Nemec, Vaclav published the artcileHighly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core, COA of Formula: C9H9BN2O2, the publication is European Journal of Medicinal Chemistry (2021), 113299, database is CAplus and MEDLINE.

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.

European Journal of Medicinal Chemistry published new progress about 1100095-25-7. 1100095-25-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (3-(1H-Pyrazol-3-yl)phenyl)boronic acid, and the molecular formula is C9H9BN2O2, COA of Formula: C9H9BN2O2.

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

Nemec, Vaclav published the artcileHighly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is European Journal of Medicinal Chemistry (2021), 113299, database is CAplus and MEDLINE.

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.

European 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

Szanto, Gabor published the artcileNew P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones, Name: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(16), 3905-3912, database is CAplus and MEDLINE.

Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clin. trials with the most advanced compound The authors have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds I is presented.

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 C23H43NP2, Name: 1H-Pyrazole-4-boronic acid.

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

Maurya, R. C. published the artcileSynthesis, characterization, thermal behavior, and DFT aspects of some oxovanadium(IV) complexes involving ONO-donor sugar Schiff bases, Safety of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Journal of Coordination Chemistry (2014), 67(18), 3084-3106, database is CAplus.

Seven new Schiff base complexes of oxovanadium(IV), [VO(L)(H₂O)], where H₂L = N-(4¹-benzoylidene-3¹-methyl-1¹-phenyl-2¹pyrazolin-5¹-one)-glucosamine (H₂bmpph-gls), N-(4¹-butyrylidene-3¹-methyl-1¹-phenyl-2¹-pyrazolin-5¹-one)glucosamine (H₂bumpph-gls), N-(3¹-methyl-1¹-phenyl-4¹-iso-valerylidene-2¹-pyrazolin-5¹-one)-glucosamine (H₂iso-vmpph-gls), N-(3¹-methyl-1¹-phenyl-4¹-propionylidene-2¹-pyrazolin-5¹-one)-glucosamine (H₂pmpph-gls) , N-(4¹-iso-butyrylidene-3¹-methyl-1¹-phenyl-2¹-pyrazolin-5¹-one)-glucosamine(H₂iso-bumpph-gls) N-(4¹-acetylidene-3¹-methyl-1¹phenyl-2¹-pyrazolin-5¹-one)-glucosamine (H₂ampph-gls), and N-(3¹-methyl-1¹-phenyl-4¹-valerylidene-2¹-pyrazolin-5¹-one)-glucosamine (H₂vmpph-gls), were synthesized by the reaction of VOSO₄.5H₂O and the said ligands in aqueous ethanol. The resulting complexes were characterized from elemental anal., vanadium determination, molar conductance, magnetic measurements, thermogravimetric (TG) anal., IR, electronic mass, and ESR studies. The thermal decomposition processes of one representative complex is discussed, and the order of reaction (n) and the activation energies (E_a) were calculated from TG and differential TG curves. Mol. geometry optimizations, mol. surface electrostatic potentials, vibrational frequency calculations, bond lengths, bond angles and dihedral angles, and natural at. charges obtained by natural bond orbital and Mulliken population anal. and calculations of mol. energies, HOMO and LUMO were performed with the Gaussian 09 software package using d. functional theory methods with Becke3-Lee-Yang-Parr (B3LYP) hybrid exchange-correlation functional and the standard 6-311G() basis set for (ampph-glsH₂) and LANL2DZ basis set for one of its complexes, [VO(ampph-gls)(H₂O)]. No imaginary frequency was found in the optimized model compounds, and hence it ensures that the mol. is in the lowest point of the potential energy surface, i.e., an energy min. Finally calculated results were applied to simulate IR spectra which show good agreement with observed spectra. Based on exptl. and theor. data, suitable square pyramidal structures are proposed for these complexes.

Journal of Coordination 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, Safety of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

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

Wang, Gary T. published the artcileLead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids, COA of Formula: C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(10), 2817-2822, database is CAplus and MEDLINE.

A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2). Small alkyl groups and 3-furyl were tolerated at the 5-position of anthranilic acid, while -OCH₃, CH₃, and Cl were found optimal for the 6-position. Placement of 2-aminoethoxy group at the 6-position enabled interaction with the second Mn²⁺ but did not result in enhancement in potency. Introduction of a tertiary amino moiety at the ortho-position of the sulfonyl Ph ring gave reduced protein binding and improved cellular activity, but led to lower oral bioavailability.

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 C6H20Cl2N4, COA of Formula: C3H5BN2O2.

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

Fernandes, Celia published the artcileRe(I) and ^99mTc(I) tricarbonyl complexes with ether-containing pyrazolyl-based chelators: Chemistry, biodistribution and metabolism, Application of 4-(methoxymethyl)-1H-pyrazole, the publication is Journal of Organometallic Chemistry (2014), 138-148, database is CAplus.

Tris(pyrazolyl)methane chelators, L1-L3, containing one or two ether groups at different positions of the azole rings, were synthesized and fully characterized. These chelators enabled the synthesis of fac-[^99mTc(CO)₃{HC[4-(ROCH₂)pz]₃}]⁺ (R = Me (Tc1), Et (Tc2)) and fac-[^99mTc(CO)₃{HC[3,5-(EtOCH₂)₂pz]₃}]⁺ (Tc3) which were identified by HPLC in comparison with the rhenium counterparts. The evaluation of Tc1-Tc3 in CD-1 mice showed that the number and/or nature of the ether groups greatly influence the biodistribution profile, pharmacokinetics and metabolic stability of these complexes. Tc1 and Tc2, bearing a unique ether substituent at the 4-position of the pyrazolyl ring, undergo metabolic transformation in vivo while Tc3 is not metabolized. The metabolization of Tc1 and Tc2 enhanced their rate of excretion but, most probably, also justify their negligible heart uptake in contrast with the high heart uptake of congener non-metabolizable complexes (^99mTc-DMEOP and ^99mTc-TMEOP), which have recently emerged as potential myocardial imaging agents. The attempts made to identify the metabolites of Tc1 and Tc2 showed that the metabolization of these compounds must involve the ether functions with probable formation of carboxylic acid derivatives A comparative study with the congener fac-[^99mTc(CO)₃{[4-(MeOCH₂)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc6) led the authors to confirm the formation of such type of metabolites. In fact, Tc6 is also metabolized in mice with formation of fac-[^99mTc(CO)₃{[4-(HOCH₂)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc7) and fac-[^99mTc(CO)₃{[4-(HOOC)pz](CH₂)₂NH(CH₂)₂NH₂}]⁺ (Tc8), which were chem. identified by HPLC in comparison with the Re congeners (Re7 and Re8).

Journal of Organometallic Chemistry 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, Application of 4-(methoxymethyl)-1H-pyrazole.

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