pyrazoles-derivatives

Di Fabio, Romano published the artcileSynthesis and Pharmacological Characterization of Novel Druglike Corticotropin-Releasing Factor 1 Antagonists, Quality Control of 3553-12-6, the publication is Journal of Medicinal Chemistry (2008), 51(23), 7370-7379, database is CAplus and MEDLINE.

To identify new CRF₁ receptor antagonists, an attempt to modify the bis-heterocycle moiety present in the top region of the dihydropyrrole[2,3]pyridine template was made following new pharmacophoric hypothesis on the CRF₁ receptor antagonists binding pocket. In particular, the 2-thiazole ring, present in the previous series of compounds, was replaced by more hydrophilic non aromatic heterocycles able to make appropriate H-bond interactions with amino acid residues Thr192 and Tyr195. This exploration, followed by an accurate anal. of the substitution of the pendant aryl ring, enabled identification of in vitro potent compounds, e.g., I, showing excellent pharmacokinetics and outstanding in vivo activity in animal models of anxiety, both in rodents and primates.

Journal of Medicinal Chemistry published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C5H7N3O, Quality Control of 3553-12-6.

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

Tereshchenkova, Anna A. published the artcileSolid-phase extraction of lanthanum on modified low-polarity sorbents, Product Details of C17H14N2O2, the publication is Vestnik Moskovskogo Universiteta, Seriya 2: Khimiya (2013), 54(4), 203-209, database is CAplus.

Preconcentration of lanthanum on various low-polarity sorbents (hexadecyl-silica, hyper cross-linked polystyrene, polyvinylidene difluoride, activated carbon) dynamically coated with 1-phenyl-3-methyl-4-benzoylpyrazol-5-one (PMBP) was studied. Reagent and lanthanum distribution coefficients were evaluated under dynamic conditions. Reagent elution was studied. Recovery of lanthanum with coated and uncoated sorbents was studied. Efficiency of desorption with nitric acid solutions or ethanol was studied.

Vestnik Moskovskogo Universiteta, Seriya 2: Khimiya 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 C10H10N2, Product Details of C17H14N2O2.

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

Arkhipova, A. A. published the artcileDifferent Approaches to Solid-Phase Extraction of Lanthanum with Low-Polar Sorbents: Comparison of Dynamic Coating, Impregnation and On-Line Mixing, SDS of cas: 4551-69-3, the publication is Separation Science and Technology (Philadelphia, PA, United States) (2015), 50(5), 729-734, database is CAplus.

Three different approaches to preconcentration of metal ions using low-polar sorbents were compared: dynamic coating of the sorbent surface with hydrophobic chelating reagent; impregnation of the sorbent with a solution of the reagent in a suitable volatile organic solvent; and online merging of sample and reagent streams prior to solid-phase extraction of metal-reagent complexes. Lanthanum was used as a model analyte; 1-phenyl-3-methyl-4-benzoylpyrazol-5-one (PMBP) as a reagent for preconcentration It was found out that the most effective approach for the analyte recovery from a large sample volume is the use of a dynamically coated sorbent with high sp. surface.

Separation Science and Technology (Philadelphia, PA, United States) 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, SDS of cas: 4551-69-3.

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

Guise, G. B. published the artcileNew approaches to washfast dyes for wool. II. Synthesis and dyeing properties of model isothiouronium dyes, Product Details of C10H9ClN2O, the publication is Journal of the Society of Dyers and Colourists (1975), 91(8), 259-64, database is CAplus.

Nine dyes with the CH2CH2SC(NH2):NH2+X- group (X = Br, iodine) were prepared and gave fast dyeings on wool in cationic form and on polyesters in disperse form (by decomposition to the thiol immediately before application). P-C6H4(NH2)2 [106-50-3] was acylated with BrCH2CH2COCl [15486-96-1], and the resulting 4-BrCH2CH2CONHC6H4NH2.HCl [57058-91-0] was diazotized and coupled with 1-(2-chlorophenyl)-3-methyl-5-pyrazolone [14580-22-4] to give an azopyrazolone, which was treated with (H2N)2CS to give I [57058-92-1]. The 8 other azo and anthraquinone dyes were prepared as described in Ger. Offen. 1,962,859 (1970). Level dyeings on wool-polyester blends could be obtained by decomposing the dye to the disperse form in an alk. bath, neutralizing, and adding more dye to give a mixture of the cationic and disperse forms. The cationic dyes also readily dyed silk, hair, and acrylic fibers, but their fastness on cellulosics was inadequate. It seems unlikely that the fastness on wool is due to formation of mixed disulfides with cystine units.

Journal of the Society of Dyers and Colourists 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

Wang, Lan published the artcileFragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors, Application In Synthesis of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(18), 4546-4552, database is CAplus and MEDLINE.

MAP4K4 has been shown to regulate key cellular processes that are tied to disease pathogenesis. In an effort to generate small mol. MAP4K4 inhibitors, a fragment-based screen was carried out and a pyrrolotriazine fragment with excellent ligand efficiency was identified. Further modification of this fragment guided by X-ray crystal structures and mol. modeling led to the discovery of a series of promising compounds with good structural diversity and physicochem. properties. These compounds exhibited single digit nanomolar potency and compounds 35 and 44 achieved good in vivo exposure.

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 C12H21NO7, Application In Synthesis of 763120-58-7.

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

Hendricks, Robert T. published the artcile3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase, Application In Synthesis of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(2), 410-414, database is CAplus and MEDLINE.

Isoquinoline-based non-nucleoside inhibitors of HCV NS5b RNA-dependent RNA-polymerase are described. The synthesis and structure-activity relationships are detailed, along with enzyme and cellular activity.

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, Application In Synthesis of 763120-58-7.

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

Annunziato, Giannamaria published the artcileInhibitors of O-Acetylserine Sulfhydrylase with a Cyclopropane-Carboxylic Acid Scaffold Are Effective Colistin Adjuvants in Gram Negative Bacteria, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Pharmaceuticals (2022), 15(6), 766, database is CAplus and MEDLINE.

Antibacterial adjuvants are of great significance, since they allow one to downscale the therapeutic dose of conventional antibiotics and reduce the insurgence of antibacterial resistance. Herein, we report that O-acetylserine sulfhydrylase (OASS) inhibitors could be used as colistin adjuvants to treat infections caused by critical pathogens spreading worldwide, Escherichia coli, Salmonella enterica serovar Typhimurium, and Klebsiella pneumoniae. Starting from a hit compound endowed with a nanomolar dissociation constant, we have rationally designed and synthesized a series of derivatives to be tested against S.Typhimurium OASS isoenzymes, StOASS-A and StOASS-B. All acidic derivatives have shown good activities in the nanomolar range against both OASS isoforms in vitro. Minimal Inhibitory Concentrations (MICs) were then evaluated, as well as compounds′ toxicity. The compounds endowed with good activity in vitro and low cytotoxicity have been challenged as a potential colistin adjuvant against pathogenic bacteria in vitro and the fractional inhibitory concentration (FIC) index has been calculated to define additive or synergistic effects. Finally, the target engagement inside the S.Typhimurium cells was confirmed by using a mutant strain in which the OASS enzymes were inactivated. Our results provide a robust proof of principle supporting OASS as a potential nonessential antibacterial target to develop a new class of adjuvants.

Pharmaceuticals 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, Recommanded Product: 1H-Pyrazole-4-boronic acid.

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

Afolabi, Fatai published the artcileSynthesis of novel heteroleptic delocalised cationic pyrazole gold complexes as potent HepG2 cytotoxic agents, Safety of 4-Bromo-1-methyl-1H-pyrazol-5-amine, the publication is Dalton Transactions (2018), 47(43), 15338-15343, database is CAplus and MEDLINE.

A new series of cationic gold(I) pyrazole complexes were prepared in excellent yields as their perchlorate salts. Results of cell viability assays show that these novel complexes have good cytotoxic properties against the human HepG2 cancer cell line. These complexes showed promising anti-cancer activities and to our knowledge, pyrazoles have never been tested against this cell line. The regioselectivity of the complexation is also discussed in regards to the substitution pattern of the pyrazoles.

Dalton Transactions published new progress about 105675-85-2. 105675-85-2 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Bromide,Amine, name is 4-Bromo-1-methyl-1H-pyrazol-5-amine, and the molecular formula is C4H6BrN3, Safety of 4-Bromo-1-methyl-1H-pyrazol-5-amine.

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

Shi, Xinzhe published the artcileC-H Bond Arylation of Pyrazoles at the β-Position: General Conditions and Computational Elucidation for a High Regioselectivity, Recommanded Product: 1-Methylpyrazole, the publication is Chemistry – A European Journal (2021), 27(17), 5546-5554, database is CAplus and MEDLINE.

Direct arylation of most five-membered ring heterocycles are generally easily accessible and strongly favored at the α-position using classical palladium-catalysis. Conversely, regioselective functionalization of such heterocycles at the concurrent β-position remains currently very challenging. Herein, authors report general conditions for regioselective direct arylation at the β-position of pyrazoles, while C-H α-position is free. By using aryl bromides as the aryl source and a judicious choice of solvent, the arylation reaction of variously N-substituted pyrazoles simply proceeds via β-C-H bond functionalization. The β-regioselectivity is promoted by a ligand-free palladium catalyst and a simple base without oxidant or further additive, and tolerates a variety of substituents on the bromoarene. DFT calculations revealed that a protic solvent such as 2-ethoxyethan-1-ol significantly enhances the acidity of the proton at β-position of the pyrazoles and thus favors this direct β-C-H bond arylation. This selective pyrazoles β-C-H bond arylation was successfully applied for the straightforward building of π-extended poly(hetero)aromatic structures via further Pd-catalyzed combined α-C-H intermol. and intramol. C-H bond arylation in an overall highly atom-economical process.

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 C18H23N3O4S, Recommanded Product: 1-Methylpyrazole.

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

Belyy, Alexander Yu. published the artcileA New Simple Procedure for the Synthesis of Heptamethyl Cyclohepta-1,3,5-triene-1,2,3,4,5,6,7-heptacarboxylate, COA of Formula: C4H6N2, the publication is Synlett (2018), 29(9), 1157-1160, database is CAplus.

A new and simple procedure for the synthesis of heptamethyl cyclohepta-1,3,5-triene-1,2,3,4,5,6,7-heptacarboxylate in a 51% yield was presented. An optimization of the reaction conditions was performed and a convenient protocol for the isolation of the reaction product was developed. The structure of the key electrophilic intermediate was determined by means of NMR spectroscopy and a plausible reaction mechanism was proposed.

Synlett 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, COA of Formula: C4H6N2.

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