Day: November 21, 2022

Yan, Li published the artcileSynthesis of tolidine-PMBP and its complexes, Recommanded Product: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Hecheng Huaxue (2012), 20(3), 386-388, database is CAplus.

Two novel Schiff bases, tolidine-PMBP (L‘) and tolidine-bisPMBP (L), were synthesized from ortho-tolidine and 1-phenyl-3-methyl-4-benzoyl-pyrazolone (PMBP) by solid method. Three complexes of L with Co(II), Cu(II) or Ni(II) were prepared The structures were characterized by UV, ¹H NMR, IR and elemental anal.

Hecheng Huaxue 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 C8H6F3NO, Recommanded Product: 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

Maurya, R. C. published the artcileDioxomolybdenum(VI) chelates of bioinorganic, catalytic, and medicinal relevance: Studies on some cis-dioxomolybdenum(VI) complexes involving O, N-donor 4-oximino-2-pyrazoline-5-one derivatives, Category: pyrazoles-derivatives, the publication is Arabian Journal of Chemistry (2015), 8(3), 293-306, database is CAplus.

A new series of five mixed-ligand complexes of dioxomolybdenum(VI) of the general composition [MoO₂(L)₂(H₂O)₂], where LH = 4-acetyloxime-3-methyl-1-phenyl-2-pyrazolin-5-one (aomppH), 3-methyl-1-phenyl-4-propionyloxime-2-pyrazolin-5-one (mppopH), 4-butyryloxime-3-methyl-1-phenyl-2-pyrazolin-5-one (buomppH), 4-iso-butyryloxime-3-methyl-1-phenyl-2-pyrazolin-5-one (ibuomppH) or 4-benzoyloxime-3-methyl-1-phenyl-2-pyrazolin-5-one (bomppH) was synthesized by the interaction of [MoO₂(acac)₂] with the said ligands in ethanol medium. The complexes so obtained were characterized by elemental analyses, molar conductance, decomposition temperature and magnetic measurements, thermogravimetric analyses, ¹H NMR, IR, mass, and electronic spectral studies. The 3D mol. modeling and anal. for bond lengths and bond angles also were carried out for one of the representative compound, [MoO₂(aomppH)₂(H₂O)₂] to substantiate the proposed structure.

Arabian 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, Category: pyrazoles-derivatives.

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

Miller, Susanne L. published the artcileC-H Borylation Catalysts that Distinguish Between Similarly Sized Substituents Like Fluorine and Hydrogen, Product Details of C4H6N2, the publication is Organic Letters (2019), 21(16), 6388-6392, database is CAplus and MEDLINE.

By modifying ligand steric and electronic profiles it is possible to C-H borylate ortho or meta to substituents in aromatic and heteroaromatic compounds, where steric differences between accessible C-H sites are small. Dramatic effects on selectivities between reactions using B₂pin₂ or 4,4,5,5-tetramethyl-1,3,2-dioxaborolane (HBpin) are described for the 1st time. Judicious ligand and borane combinations give highly regioselective C-H borylations on substrates where typical borylation protocols afford poor selectivities.

Organic 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, Product Details of C4H6N2.

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

Qiao, Lixin published the artcileStructure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors, Application of Pyrazolo[1,5-a]pyridin-3-amine, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(21), 6122-6126, database is CAplus and MEDLINE.

A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a Ph or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful mol. probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.

Bioorganic & Medicinal Chemistry Letters published new progress about 137837-55-9. 137837-55-9 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Amine, name is Pyrazolo[1,5-a]pyridin-3-amine, and the molecular formula is C7H7N3, Application of Pyrazolo[1,5-a]pyridin-3-amine.

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

Hemshekhar, Mahadevappa published the artcileHost defense peptide LL-37-mediated chemoattractant properties, but not anti-inflammatory cytokine IL-1RA production, is selectively controlled by Cdc42 Rho GTPase via G protein-coupled receptors and JNK mitogen-activated protein kinase, Computed Properties of 71203-35-5, the publication is Frontiers in Immunology (2018), 1871/1-1871/17, database is CAplus and MEDLINE.

The human host defense peptide LL-37 promotes immune activation such as induction of chemokine production and recruitment of leukocytes. Conversely, LL-37 also medi-ates anti-inflammatory responses such as production of anti-inflammatory cytokines, e.g., IL-1RA, and the control of pro-inflammatory cytokines, e.g., TNF. The mechanisms regulating these disparate immunomodulatory functions of LL-37 are not completely understood. Rho GTPases are GTP-binding proteins that promote fundamental immune functions such as chemokine production and recruitment of leukocytes. However, recent studies have shown that distinct Rho proteins can both neg. and pos. regulate inflammation. Therefore, we interrogated the role of Rho GTPases in LL-37-mediated immunomodulation. We demonstrate that LL-37-induced production of chemokines, e.g., GRO-α and IL-8 is largely dependent on Cdc42/Rac1 Rho GTPase, but indepen-dent of the Ras pathway. In contrast, LL-37-induced production of the anti-inflammatory cytokine IL-1RA is not dependent on either Cdc42/Rac1 RhoGTPase or Ras GTPase. Functional studies confirmed that LL-37-induced recruitment of leukocytes (monocytes and neutrophils) is also dependent on Cdc42/Rac1 RhoGTPase activity. We demonstrate that Cdc42/Rac1-dependent bioactivity of LL-37 involves G-protein-coupled receptors (GPCR) and JNK mitogen-activated protein kinase (MAPK) signaling, but not p38 or ERK MAPK signaling. We further show that LL-37 specifically enhances the activity of Cdc42 Rho GTPase, and that the knockdown of Cdc42 suppresses LL-37-induced production of chemokines without altering the peptide’s ability to induce IL-1RA. This is the first study to demonstrate the role of Rho GTPases in LL-37-mediated responses. We demonstrate that LL-37 facilitates chemokine production and leukocyte recruitment engaging Cdc42/Rac1 Rho GTPase via GPCR and the JNK MAPK pathway. In contrast, LL-37-mediated anti-inflammatory cytokine IL-1RA production is independent of either Rho or Ras GTPase. The results of this study suggest that Cdc42 Rho GTPase may be the mol. switch that controls the opposing functions of LL-37 in the process of inflammation.

Frontiers in Immunology published new progress about 71203-35-5. 71203-35-5 belongs to pyrazoles-derivatives, auxiliary class GPCR/G Protein,Ras, name is 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C22H21N3O3S, Computed Properties of 71203-35-5.

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

Pfefferkorn, Jeffrey A. published the artcileP2Y₁ receptor antagonists as novel antithrombotic agents, Related Products of pyrazoles-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(11), 3338-3343, database is CAplus and MEDLINE.

The P2Y₁ and P2Y₁₂ purinergic receptors are responsible for mediating ADP (ADP) dependent platelet aggregation. Evidence from P2Y₁ knockout studies as well as from nucleotide-based small mol. P2Y₁ antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y₁ antagonists that are potent and orally bioavailable.

Bioorganic & Medicinal Chemistry Letters 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, Related Products of pyrazoles-derivatives.

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

Skinner, Philip J. published the artcileFluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a, Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(20), 5620-5623, database is CAplus and MEDLINE.

A series of 5-alkyl pyrazole-3-carboxylic acids, e.g., I, were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.

Bioorganic & Medicinal Chemistry 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 C17H14N2O2, Application of 3-Isopropyl-1H-pyrazole-5-carboxylic acid.

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

Yu, Hui published the artcileSynthesis, characterization and properties of rare earth complexes with pyrazolone and 2,6-pyridinecarboxylic acid, Application In Synthesis of 4551-69-3, the publication is Zhongguo Xitu Xuebao (2014), 32(3), 328-337, database is CAplus.

The four new solid ternary complexes of rare earth with 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone and 2,6-pyridinecarboxylic acid, Na₂[RE(PMBP)₃(PDA)]·nH₂O (RE = Sm³⁺, Y³⁺, Er³⁺, the La-complex including one coordinated water), were synthesized and characterized by elemental anal., FTIR, UV-visible, XRD, TG-DTA and XPS. The antibacterial activities test indicated that all the complexes exhibited moderate antibacterial ability against Escherichia coli and Staphylococcus aureus. also studied the interactions of the Er-complex with calf thymus DNA (CT DNA) employing florescence spectroscopic and UV spectrum. DNA interaction studies suggested the Er-complex could intercalate between DNA base pairs. The Sm-complex might be used as fluorescent probe.

Zhongguo Xitu Xuebao 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 C6H13I, Application In Synthesis of 4551-69-3.

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

Zhu, You-Quan published the artcileDesign, synthesis and quantitative structure-activity relationship study of herbicidal of 3,4-dihydro-3-phenyl-4-oxopyrazolo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid ethyl ester derivatives, Safety of Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, the publication is Youji Huaxue (2008), 28(6), 1044-1049, database is CAplus.

A method for the synthesis of the title compounds [i.e., 4-ethoxycarbonyl-1,7-dihydro-1-(substituted phenyl)-5-(un)substituted pyrazolo[5,1-d][1,2,3,5]tetrazin-7-one derivatives] is reported here. Their structures were confirmed by ¹H NMR, IR spectra and elemental anal. A bioassay results showed that these compounds exhibited herbicidal activity. Quant. structure-activity relationship studies showed that their herbicidal activity was correlated with the molar refractivity (MR; optical refraction, molar refraction) and steric or hydrophobic physicochem. parameters, where the correlation coefficients were larger than 0.8. The herbicidal activity against Brassica campestris (Brassica rapa) was mainly affected by the MR for Ph substituents and the hydrophobic parameter (π) for the substituent on the pyrazolo[5,1-d]-1,2,3,5-tetrazine group. When MR was about 1.452, the compound showed the highest herbicidal activity. The herbicidal activity against Echinochloa crus-galli was mainly related with Taft (Es) for the ortho-Ph substituent and the hydrophobic parameter (π) for the ortho-substituents and meta-substituents.

Youji Huaxue 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 C13H15NO6S, Safety of Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate.

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

Li, Yingjun published the artcileN-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors, Related Products of pyrazoles-derivatives, the publication is ACS Medicinal Chemistry Letters (2015), 6(5), 543-547, database is CAplus and MEDLINE.

A series of N-(3-ethynyl-2,4-difluorophenyl)sulfonamides were identified as new selective Raf inhibitors. The compounds potently inhibit B-Raf^V600E with low nanomolar IC₅₀ values and exhibit excellent target specificity in a selectivity profiling investigation against 468 kinases. They strongly suppress proliferation of a panel of human cancer cell lines and patient-derived melanoma cells with B-Raf^V600E mutation while being significantly less potent to the cells with B-Raf^WT. The compounds also display favorable pharmacokinetic properties with a preferred example (3s) demonstrating significant in vivo antitumor efficacy in a xenograft mouse model of B-Raf^V600E mutated Colo205 human colorectal cancer cells, supporting it as a promising lead compound for further anticancer drug discovery.

ACS Medicinal Chemistry Letters published new progress about 1363381-82-1. 1363381-82-1 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Bromide,Ether, name is 5-Bromo-3-methoxy-1H-pyrazolo[3,4-b]pyridine, and the molecular formula is C7H6BrN3O, Related Products of pyrazoles-derivatives.

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