99853-56-2

Upstream product

• 20629-92-9 1-(4-chlorophenyl)-3-methyl-3-pyrazolin-5-one 
• 77-78-1 dimethyl sulfate 
• 74-83-9 methyl bromide 
• 13024-90-3 1-(4-chlorophenyl)-3-methyl-2-pyrazolin-5-one 
• 74-88-4 methyl iodide 
• 1073-70-7 4-chlorophenylhydrazine hydrochloride 
• 1073-69-4 N-4-chlorophenylhydrazine 

Relevant academic research and scientific papers

Pd(ii)-Catalyzed alkyne annulation through allylic isomerization: synthesis of spiro-cyclopentadiene pyrazolones

The Pd(ii)-catalyzed activation of Csp2-H bond and double alkyne annulation which proceedsviaallylic isomerization is reported for the first time. This reaction of antipyrines with alkynes provides an efficient synthetic route for the biologically important spiro-cyclopentadiene pyrazolones. In the presence of Lawesson's reagent, this Pd(ii)-catalyzed annulation reaction affords another spiro-cyclopentadiene pyrazolone which displays very good fluorescence properties.

SCREENING METHODS AND THERAPEUTIC APPLICATIONS BASED ON BACTERIAL MOTILITY INHIBITION

The present invention relates to compounds for use in treating and/or preventing a bacterial infection or a condition associated with the bacterial infection, wherein the bacterial infection is caused by flagellated bacteria. The present invention further relates to a method of identifying compounds having bacterial anti-motility activity.

The selective condensation of pyrazolones to isatins in aqueous medium

The selective condensation of pyrazolones with isatins using water as the reaction medium is presented. This strategy provides an environmentally benign synthetic route to synthesize various potentially bioactive pyrazolone substituted oxindoles.

Copper-catalyzed acylation of pyrazolones with aldehydes to afford 4-acylpyrazolones

Copper-catalyzed direct acylation of the alkenyl C-H bond in 1,2-dihydro-3H-pyrazol-3-ones has been developed, affording a series of 4-acylpyrazolones in moderate to good yields. Notably, this protocol involves readily accessible substrates and reagents, which have good functional group tolerance leading to pyrazolone derivatives under mild reaction conditions.

Pyrazolone derivatives: Synthesis, anti-inflammatory, analgesic quantitative structure-activity relationship and in vitro studies

Some 1-(4-chlorophenyl or benzenesulfonamide)-2,3- and/or 4-substituted-1H-pyrazol-5(4H)-one derivatives were synthesized and screened for their anti-inflammatory and analgesic activities, in addition to their ulcerogenic liability. They were found to be active as anti-inflammatory and analgesic agents. Compound 6b was found to be the most active as anti-inflammatory agent and compound 9b was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, cyclooxygenase-1/-2 (COX-1)/COX-2 isozyme selectivity was also done and the tested compounds showed equal inhibition to both isoforms. Moreover, 2D-quantitative structure-activity relationship (QSAR) studies revealed well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds.

Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists

The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.

PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS

Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.