39848-01-6

Upstream product

• 67-56-1 methanol 
• 55991-68-9 5-(p-tolyl)-2,3-dihydro-2,3-furandione 
• 113416-20-9 (Z)-4-Oxo-2-phenylamino-4-p-tolyl-but-2-enoic acid methyl ester 
• 122-00-9 para-methylacetophenone 
• 95-92-1 oxalic acid diethyl ester 
• 553-90-2 Dimethyl oxalate 

Downstream Products

• 113416-20-9 (Z)-4-Oxo-2-phenylamino-4-p-tolyl-but-2-enoic acid methyl ester 
• 178408-22-5 3-(2-oxo-2-p-tolyl-ethylidene)-1-phenyl-piperazin-2-one 
• 510713-41-4 5-(4-ethylphenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 440108-83-8 3-hydroxy-5-(4-hydroxyphenyl)-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 1276115-54-8 3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-5-(4-trifluoromethoxyphenyl)-1,5-dihydropyrrol-2-one 
• 1276115-55-9 3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-5-(4-trifluoromethylphenyl)-1,5-dihydropyrrol-2-one 
• 1276115-56-0 3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-5-(3-trifluoromethylphenyl)-1,5-dihydropyrrol-2-one 
• 1276115-57-1 5-(2,4-bis-trifluoromethylphenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 1276115-58-2 5-(3,5-bis-trifluoromethylphenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 459795-47-2 5-(4-chlorophenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 1276115-59-3 5-(3-chlorophenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 1276115-60-6 5-(3,5-dichlorophenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 1276115-61-7 5-(4-chloro-3-trifluoromethylphenyl)-3-hydroxy-1-(2-hydroxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 
• 433258-01-6 3-hydroxy-5-(4-isopropylphenyl)-1-(3-methoxypropyl)-4-(4-methylbenzoyl)-1,5-dihydropyrrol-2-one 

Relevant academic research and scientific papers

Design, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives

According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives (6aa–6gc) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids with secnidazole. The in vi

Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition

The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with c

Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX

In our previous study, we designed a series of pyrazole derivatives as novel COX-2 inhibitors. In order to obtain novel dual inhibitors of COX-2 and 5-LOX, herein we designed and synthesized 20 compounds by hybridizing pyrazole with substituted coumarin w

Design, synthesis and evaluation of benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives as COX-1/COX-2 agents against solid tumors

Novel benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives have been designed, synthesized and evaluated for their biological activities as selective COX-2 inhibitors with anticancer potential. In vitro the bioass

Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis

Cyclooxygenase-2 is frequently overexpression in malignant tumors and the product PGE2promotes cancer cell progression and metastasis. We designed novel series of coumarin sulfonamides derivatives to improve biological activities of COX-2 inhib

Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation

As an important enzyme in bacterial protein biosynthesis, tyrosyl-tRNA synthetase (TyrRS) has been an absorbing therapeutic target for exploring novel antibacterial agents. A series of metronidazole-based antibacterial agents has been synthesized and iden

Design, synthesis, and structure-activity relationship exploration of 1-substituted 4-aroyl-3-hydroxy-5-phenyl-1 H -pyrrol-2(5 H)-one analogues as inhibitors of the annexin A2′S100A10 protein interaction

S100 proteins are small adaptors that regulate the activity of partner proteins by virtue of direct protein interactions. Here, we describe the first small molecule blockers of the interaction between S100A10 and annexin A2. Molecular docking yielded cand

Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids: Synthesis, nitric oxide release studies and anti-inflammatory activities

A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs) wherein an O2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate (11a-c) NO-donor moiety is attached directly to the carboxylic acid group of 1-(4-methanesulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids were synthesized. The diazen-1-ium-1,2-diolate compounds 11a-c all released a low amount of NO upon incubation with phosphate buffer (PBS) at pH 7.4 (7.7-9.3% range). In comparison, the percentage of NO released was significantly higher (67.5-73.6% of the theoretical maximal release of two molecules of NO/molecule of the parent hybrid ester prodrug) when the diazen-1-ium-1,2-diolate ester prodrugs were incubated in the presence of rat serum. These incubation studies suggest that both NO and the anti-inflammatory 1-(4-methanesulfonylphenyl)-5-(4-H, 4-F or 4-Me-phenyl)-1H-pyrazol-3-carboxylic acid (9a-c) would be released from the parent NONO-coxib upon in vivo cleavage by non-specific serum esterases. The 1-(4-methanesulfonylphenyl)-5-(4-H, 4-F or 4-Me-phenyl)-1H-pyrazol-3-carboxylic acids (9a-c) exhibited AI activities (ID50 = 85.2-104.4 mg/kg po range) between that exhibited by the reference drugs aspirin (ID50 = 128.7 mg/kg po) and celecoxib (ID50 = 10.8 mg/kg po). Hybrid ester anti-inflammatory/NO-donor prodrugs (NONO-coxibs) offers a potential drug design concept targeted toward the development of anti-inflammatory drugs that are devoid of adverse ulcerogenic and/or cardiovascular effects.

Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids and esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: Potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents

The synthesis and structure-activity relationship of a series of 4-aryl- 2-hydroxy-4-oxobut-2-enoic acids and esters and 2-amino-4-aryl-4-oxobut-2- enoic acids and esters as potent inhibitors of kynurenine-3-hydroxylase are described. These compounds are

Study of the Mechanisms of Reactions of 1,3-Dicarbonyl Compounds with Nucleophilic Reagents: X. Kinetics of the Hydrolysis of Methyl 4-Aryl-2-Arylamino-4-Oxobut-2-Enoates

The kinetics of hydrolysis of methyl 4-aryl-2-arylamino-4-oxobut-2-enoates in 50% aqueous dioxane in the presence of acetate and monochloroacetate buffer solutions was studied by spectrophotometry. An analysis of the dependence of the rate of hydrolysis on the concentrations and the composition of the components of the solutions and on the nature of the substituents in the substrate made it possible to propose a mechanism of general acid catalysis of the reaction.