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.
The mechanism of formation of 6-aryl-4,6-dioxohexanoic acids from arylketones and succinic anhydride
Compounds 2a-d could be synthesized directly from the requisite acetophenone enolate and succinic anhydride. Intermediate O-acylated products 1a-d were observed. Compounds 1a-d could be converted to 2a-d by treatment with at least two additional equivalen
Murray, William V.,Lalan, Praful,Connolly, Peter J.
p. 5189 - 5192
(2007/10/02)
Synthesis and Properties of Aryl-1,3-dioxo Carboxylic Acids
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Murray, William V.,Wachter, Michael P.
p. 3424 - 3426
(2007/10/02)
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