56872-21-0

Upstream product

• 39496-87-2 4-(3-chloro-4-methoxyphenyl)-4-oxobutanoic acid 
• 108-30-5 succinic acid anhydride 
• 95-57-8 2-monochlorophenol 
• 766-51-8 2-Chloroanisole 

Downstream Products

• 56872-23-2 methyl 3-(3-chloro-4-hydroxybenzoyl)propionate 
• 100119-67-3 4-(3-chloro-4-methoxy-phenyl)-4-oxo-butyric acid methyl ester 
• 74362-74-6 4-(3-Chloro-4-isopropoxy-phenyl)-4-oxo-butyric acid 
• 1456819-45-6 6-(3-chloro-4-hydroxy-phenyl)-2-(p-(methanesulfonyl)phenyl)-4,5-dihydropyridazi-3(2H)-one 

Relevant academic research and scientific papers

Synthesis, antiproliferative and anti-inflammatory activities of some novel 6-aryl-2-(p-(methanesulfonyl)phenyl)-4,5-dihydropyridazi-3(2H)-ones

Sixteen new 6-aryl-2-(p-(methanesulfonyl)phenyl)-4,5-dihydropyridazi-3(2 H)-ones (2a-p) were synthesized and tested for in vitro anticancer and in vivo anti-inflammatory activities. Eleven (2b, 2d , 2-ej and 2m-p) of the obtained compounds were screened for their antiproliferative activity towards 60 human cancer cell lines by the National Cancer Institute (USA). Compound 2f showed remarkable activity with GI50 less than 1 μM on 36 human tumor cell lines and has been referred to Biological Evaluation Committee (NCI) for advance study. Compound 2g also displayed promising antiproliferative activity against 20 different cell lines with GI50 less than 1 μM. Compounds 2k and 2n were found to have a comparable anti-inflammatory activity to that of standard drug etoricoxib in carrageenan-induced rat hind paw edema model at 5 h.

Syntheses and antiinflammatory activity of some 6-aryl-2,3,4,5-tetrahydro-3-pyridazinones

6-Aryl-2, 3, 4, 5-tetrahydro-3-pyridazinones (2c-22c) are obtained by dehydrocyclisation of various hydrazides formed by the reaction of appropriate methyl β-aroylpropionate and hydrazine hydrate in the presence of anhydrous sodium acetate. They show promising antiinflammatory activity during their evaluation by carrageenin induced paw edema test in rats.

ON THE QUANTITATIVE RELATIONS BETWEEN STRUCTURE AND ANTIAGGREGATION ACTIVITY OF ω-ARYL-ω-OXOALKANOIC ACIDS

A series of ω-aryl-ω-oxoalkanoic acids, I-IV, has been prepared and investigated for dissociation constants in 80percent methylcellosolve, retention characteristics in thin-layer partition chromatography and partition coefficients P in the system octanol-water.Also evaluated were their anti-inflammatory efficacy and inhibitory effect on the platelet aggregation induced by collagen.Analysing the relations between structure and antiaggregation effect, we obtained a non-linear, quadratic dependence of this effect on lipophilicity, the optimum being at log P = 3.The antiaggregation effect increased with shortening the chain between the carbonyl and the carboxyl, and with increasing acidity.It was also diminished by the presence of a methyl group on the interlinking chain.To assess the role of lipophilicity we used the RM values of partition chromatography.The relation between anti-inflammatory efficacy and structure was assessed only qualitatively.In this aspect, too, the nature of the chain between the carbonyl and carboxyl proved to have a marked influence.The anti-inflammatory activity proved considerably enhanced by the presence of another aromatic ring in ω-oxoalkanoic acids derived from biphenyl.

6-(3-SUBSTITUTED AMINO-2-HYDROXYPROPOXYARYL)-4,5-DIHYDRO-3(2H)-PYRIDAZINONES

The compounds are 6-(3-substituted amino-2-hydroxypropoxyaryl)-4,5-dihydro-3(2H)-pyridazinones which are β-adrenergic blocking agents.