Day: November 15, 2022

Mathur, J. N. published the artcileThermodynamics of americium(3+)-substituted pyrazolone-crown ether adducts, COA of Formula: C12H9F3N2O2, the main research area is americium pyrazolone crown ether adduct.

The thermodn. parameters for the extraction of Am3+ with pyrazolones (HA = HPMBP or HPMTFP) alone as well as their mixtures with one of the crown ethers B15C5 or DCH18C6 were calculated in chloroform at 30° by using the temperature coefficient method. The self-adduct species Am(A)3.HA is enthalpy stabilized. The adduct species Am(A)3.HA.DCH18C6 are stabilized by entropy and opposed by enthalpy. The adduct species Am(A)3.HA.B15C5 (HA = HPMBP) and Am(A)3.B15C5 or Am(A)3.2B15C5 (HA = HPMTFP) are stabilized by enthalpy. These data were correlated with the difference in the nature of binding of the two crown ethers with Am3+.

Solvent Extraction and Ion Exchange published new progress about Complexation enthalpy. 1691-93-6 belongs to class pyrazoles-derivatives, name is 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one, and the molecular formula is C12H9F3N2O2, COA of Formula: C12H9F3N2O2.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elfahham, Hassan A. published the artcileThe reactions of nitrile imines with amino- and oxo-substituted azoles, Name: 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is azole reaction nitrile imine hydrazonyl halide; pyrazole cyclization hydrazonyl chloride; pyrazolopyrazole; pyrazolotriazole; azatricycloundecanone; adamantanone oxime rearrangement.

The behavior of several amino and hydroxy azoles toward nitrile imines and hydrazonyl halides is reported. Thus, the pyrazoles I (R = Ph, R1 = H2N, OH) reacted with PhCCl:NNHPh to give the pyrazolopyrazole II. I (R = Me, R1 = OH) under identical conditions gave the pyrazolotriazole III. I (R = Ph, R1 = NH2) reacted with MeCOCCl:NNHPh to give the pyrazoloimidazole IV.

Chemistry Letters published new progress about Cycloaddition reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Name: 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Nishioka, Masanori published the artcileInduction of resistance against rice blast disease by a novel class of plant activator, pyrazolecarboxylic acid derivatives, Category: pyrazoles-derivatives, the main research area is pyrazolecarboxylate derivative preparation rice blast disease resistance.

Synthesis and characterization of anti-rice blast activity of pyrazole derivatives was described. Structure-activity relationship study indicated that a carboxyl group at 5-position of 1-methyl-1H-pyrazole played an important role in the activity and that a halogen atom such as a chlorine or bromine at 3-position enhanced the activity. Among the derivatives, 3-chloro-1-methyl-1H-pyrazole-5-carboxylic acid (CMPA) exhibited the highest anti-rice blast activity with the ED80 (80% ED, the concentration needed for 80% inhibition of disease development) of 0.05 mg/pot. CMPA did not have any significant effects on the hyphal growth, spore germination, and appressorium formation of Pyricularia oryzae, suggesting that CMPA induces systemic acquired resistance in rice plants.

Journal of Pesticide Science (Tokyo, Japan) published new progress about Agrochemical fungicides. 63425-54-7 belongs to class pyrazoles-derivatives, name is 3-Chloro-1-methyl-1H-pyrazole, and the molecular formula is C4H5ClN2, Category: pyrazoles-derivatives.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Nwankwoala, Reginaid N. P. published the artcileAnti inflammatory property of new pyrazolon derivatives, Safety of 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one, the main research area is antiinflammatory inflammation pyrazolone derivative phenylbutazone.

The anti inflammatory effects of 4-trifluoroacety1-1-pheny1-3-methy1 pyrazolone (HTFP) and 4-sebacyl-1-bis 1-pheny1-3-methy1 pyrazolone (HSP) were investigated and compared with those of phenylbutazone (PTZ) using carrageenan-induced paw inflammation model in rats. Different doses of PTZ, HTFP and HSP were intra-peritoneally administered to rats and one hour thereafter, inflammation was induced by injecting carrageenan into the left foot of the rat. The right foot received saline. Five (5) rats received carrageenan and saline only. Both the left and right feet were measured hourly for four hours. PTZ, HTFP and HSP significantly reduced carrageenan induced inflammation. 100Mg/kg PTZ caused 62.5 ± 5.25% reduction of the inflammatory response whereas 10mg/kg HTFP and 10mg/kg HSP reduced inflammatory response by 53.6 ± 5.0% and 32.5 ± 4.50% resp. Thus anti-inflammatory properties of these drugs were less at lower doses. These results show that (1) HTFP and HSP possess anti-inflammatory property, (2) HTFP is more potent than HSP and (3) The anti-inflammatory potency of phenylbutazone drug is greatly enhanced by substitution of trifluoroacety1-1-group at position 4 of the pyrazolone mol.

Research Journal of Medicine and Medical Sciences published new progress about Anti-inflammatory agents. 1691-93-6 belongs to class pyrazoles-derivatives, name is 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one, and the molecular formula is C12H9F3N2O2, Safety of 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

McElroy, William T. published the artcilePotent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation, Recommanded Product: tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate, the main research area is preparation amidopyrazole inhibitor IRAK4 inflammation structure; Interleukin-1 receptor-associated kinase 4; SAR; drug discovery; inflammation; structure-based drug design.

IRAK4 is a critical upstream kinase in the IL-1R/TLR signaling pathway. Inhibition of IRAK4 is hypothesized to be beneficial in the treatment of autoimmune related disorders. A screening campaign identified a pyrazole class of IRAK4 inhibitors that were determined by X-ray crystallog. to exhibit an unusual binding mode. SAR efforts focused on the identification of a potent and selective inhibitor with good aqueous solubility and rodent pharmacokinetics. Pyrazole C-3 piperidines were well tolerated, with N-sulfonyl analogs generally having good rodent oral exposure but poor solubility N-Alkyl piperidines exhibited excellent solubility and reduced exposure. Pyrazoles possessing N-1 pyridine and fluorophenyl substituents were among the most active. Piperazine 32 was a potent enzyme inhibitor with good cellular activity. Compound 32 reduced the in vivo production of proinflammatory cytokines and was orally efficacious in a mouse antibody induced arthritis disease model of inflammation.

ACS Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 1169563-99-8 belongs to class pyrazoles-derivatives, name is tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate, and the molecular formula is C13H22N4O2, Recommanded Product: tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Mugnaini, Claudia published the artcileDesign, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity In Vivo, Quality Control of 637336-53-9, the main research area is hydroxy oxopyrazolopyridine carboxamide preparation antiosteoarthritic osteoarthritis cannabinoid type receptor.

The hallmark of joint diseases, such as osteoarthritis (OA), is pain, originating from both inflammatory and neuropathic components, and compounds able to modulate the signal transduction pathways of the cannabinoid type-2 receptor (CB2R) can represent a helpful option in the treatment of OA. In this perspective, a set of 18 cannabinoid type-2 receptor (CB2R) ligands was developed based on an unprecedented structure. With the aim of improving the physicochem. properties of previously reported 4-hydroxy-2-quinolone-3-carboxamides, a structural optimization program led to the discovery of isosteric 7-hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide derivatives These new compounds are endowed with high affinity for the CB2R and moderate to good selectivity over the cannabinoid type-1 receptor (CB1R), associated with good physicochem. characteristics. As to the functional activity at the CB2R, compounds able to act either as agonists or as inverse agonists/antagonists were discovered. Among them, compound I emerged as a potent CB2R agonist able to reduce pain in rats carrying OA induced by injection of monoiodoacetic acid (MIA).

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 637336-53-9 belongs to class pyrazoles-derivatives, name is Methyl 4-amino-1-methyl-1H-pyrazole-3-carboxylate, and the molecular formula is C6H9N3O2, Quality Control of 637336-53-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elfahham, H. A. published the artcileSynthesis of heterocycles through the reactions of nitrilimines with amino and oxo diazoles, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is pyrazoletriazole; pyrazolopyrazine; pyrazoloimidazole; nitrilimine cyclocondensation diazole; pyrazole amino hydroxy cyclocondensation nitrilimine.

Fused azoles such as pyrazolo[5,1-c][1,2,4]triazoles, pyrazolo[3,4-b]pyrazine and pyrazolo[1,5-a]imidazole have been prepared from the reactions of nitrilimines , produced from hydrazidoyl halides I (R = Cl, Me, MeO), or II (R1 = NO2, Me), with amino- and oxo-azoles. In some cases acyclic products are formed.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Cyclocondensation reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Mugnaini, Claudia published the artcileSynthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease, HPLC of Formula: 637336-53-9, the main research area is adamantanylcarboxamidothiophene preparation cannabinoid 2 receptor agonist skin inflammation; CB2R agonists; CBR ligands; Chemokine release; Skin inflammation.

A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist Me 2-[((adamantan-1-yl)carbonyl)amino]-4-ethyl-5-methylthiophene-3-carboxylate , showing the best balance between receptor affinity and selectivity, was tested in vitro in an exptl. model of allergic contact dermatitis and is able to block the release of MCP-2 in HaCaT cells at 10 μM concentration

European Journal of Medicinal Chemistry published new progress about Allergic contact dermatitis. 637336-53-9 belongs to class pyrazoles-derivatives, name is Methyl 4-amino-1-methyl-1H-pyrazole-3-carboxylate, and the molecular formula is C6H9N3O2, HPLC of Formula: 637336-53-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Hecht, Sidney M. published the artcileActivation of cytokinins, Quality Control of 54385-49-8, the main research area is cytokinin analog structure activity; plant hormone cytokinin analog.

A number of cytokinin analogs containing modifications in the heterocyclic moiety were prepared These compounds were tested for activity as cytokinins and anticytokinins in the tobacco bioassay and the results were used to determine whether any position(s) of the heterocyclic nucleus of cytokinins may require derivatization as part of an over-all activation process. 3-Substituted 4-alkylaminopyrazolo[3,4-d]pyrimidines and 4-alkylaminopyrrolo[2,3-d]pyrimidines, have carbon rather than nitrogen atoms at positions 3 and 5, resp., (analogous to position 7 in purines) and would be predicted to be metabolically stable at these positions. The finding that these compounds had cytokinin activity suggested that modification at the metabolically stable position, and by extension at position 7 in cytokinin analogs which are purines, is not a prerequisite for the expression of cytokinin activity. Similar consideration of other heterocyclic analogs which have cytokinin activity suggests that the active form of a cytokinin can be the exogenous compound itself. Certain structural analogs of cytokinins were found to inhibit the growth of tobacco callus promoted by 6-(3-methyl-2-butenylamino)purine. These compounds were studied as potential cytokinin antagonists, i.e. having activity analogous to the 7-alkylamino-3-methylpyrazolo[4,3-d]pyrimidines (Hecht, S. M., Bock, R. M., Schmitz, R. Y., Skoog, F., and Leonard, N. J. 1971; Skoog, F., Schmitz, R. Y., Hecht, S. M., and Bock, R. M. 1973). The activity of these compounds is discussed and criteria are proposed to distinguish between those species which are specific anticytokinins and those which otherwise inhibit growth.

Journal of Biological Chemistry published new progress about Structure-activity relationship. 54385-49-8 belongs to class pyrazoles-derivatives, name is 5-Amino-1H-pyrazole-3,4-dicarbonitrile, and the molecular formula is C5H3N5, Quality Control of 54385-49-8.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Modi, C. K. published the artcileSynthetic, spectroscopic and thermal aspects of some heterochelates, Recommanded Product: 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one, the main research area is transition metal pyrazolylethylideneaminobenzoate benzylideneethylenediamine preparation; reaction kinetics activation energy thermolysis transition metal pyrazolylethylideneaminobenzoate benzylideneethylenediamine; activation entropy enthalpy thermolysis transition metal pyrazolylethylideneaminobenzoate benzylideneethylenediamine; free energy thermolysis transition metal pyrazolylethylideneaminobenzoate benzylideneethylenediamine.

The present article describes the synthesis, structural features and thermal studies of heterochelates [M(SB)(benen)(H2O)]·nH2O [where H2SB = (Z)-2-(2,2,2-trifluoro-1-(5-hydroxy-3-methyl-1-phenyl-1H-pyrazol-4-yl)ethylideneamino)benzoic acid, benen = bis(benzylidene)ethylenediamine and M = Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and VO(IV)]. The Schiff base (H2SB) was characterized from elemental anal., IR, 1H and 13C NMR. The heterochelates were characterized from elemental analyses, magnetic measurements, solid state conductivity measurements, IR, reflectance spectra, and thermal studies. The FAB mass spectrum of [Co(SB)(benen)(H2O)] was carried out. The kinetic parameters such as order of reaction (n) and the energy of activation (Ea) are reported using Freeman-Carroll method. The pre-exponential factor (A), the activation entropy (ΔS#), the activation enthalpy (ΔH#) and the free energy of activation (ΔG#) were calculated

Journal of Thermal Analysis and Calorimetry published new progress about Activation energy (thermolysis). 1691-93-6 belongs to class pyrazoles-derivatives, name is 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one, and the molecular formula is C12H9F3N2O2, Recommanded Product: 5-Methyl-2-phenyl-4-(2,2,2-trifluoroacetyl)-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics