1087032-91-4

Upstream product

• 111881-78-8 6-(4-chlorophenyl)-4,6-dioxohexanoic acid 
• 99-91-2 para-chloroacetophenone 

Downstream Products

• 1443778-00-4 3-(5-(4-chlorophenyl)-1-(6-methoxypyridazin-3-yl)-1Hpyrazol-3-yl)-1-morpholinopropan-1-one 
• 1443777-99-8 3-(5-(4-chlorophenyl)-1-(6-methoxypyridazin-3-yl)-1Hpyrazol-3-yl)-1-(piperidin-1-yl)propan-1-one 

Relevant academic research and scientific papers

Pyrazole derivatives as inhibitors of arachidonic acid-induced platelet aggregation

Antiplatelet drugs are promising therapeutics to intervene with platelet aggregation in arterial thrombosis, most prominently in myocardial infarction and ischemic stroke. Here, we describe the synthesis and structure-activity relationships of potent inhibitors of platelet aggregation based on the 1,5-diarylpyrazol-3-carboxamide scaffold. Analogs from this series demonstrated potent anti-aggregatory activities against arachidonic acid-induced platelet aggregation, as measured by turbidimetric method of Born. 1,5-Diarylpyrazole-3- carboxamides obtained with small-basic amines (7, 8, 50, 51, 61, 62) displayed the strongest activity with IC50 values in low nanomolar range (5.7-83 nM). On the basis of their high potency in cellular environment, these straightforward pyrazole derivatives may possess potential in the design of more potent compounds for intervention with cardiovascular diseases.

Synthesis of 1,5-diarylpyrazol-3-propanoic acids towards inhibition of cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4 formation

A set of 25 derivatives of 3-[1-(6-substituted-pyridazin-3-yl)-5-(4- substitutedphenyl)-1H-pyrazol-3-yl]propanoic acids has been synthesized and evaluated for their in vitro cyclooxygenase-1/2 (COX-1/ 2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes as well as for their 5-lipoxygenase (5-LO)-mediated LTB4 formation inhibitory activity using an assay with activated human polymorphonuclear leukocytes (PMNL). Among the synthesized compounds, especially 4g showed COX-1 (IC50 = 1.5 μM) and COX-2 (IC50 = 1.6 μM) inhibitory activity, whereas compounds 4b and 4 f resulted in the inhibition of 5-LO-mediated LTB4 formation at 14 μM and 12 μM IC50 values, respectively, without any significant inhibition on COX isoforms. ECV · Editio Cantor Verlag.