1254703-85-9Relevant academic research and scientific papers
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis
Abay, Efrem,Barry, Clifton E.,Basarab, Gregory S.,Boshoff, Helena I. M.,Boyle, Grant A.,Chibale, Kelly,Eyermann, Charles J.,Fienberg, Stephen,Ghorpade, Sandeep R.,Khonde, Lutete Peguy,Lawrence, Nina,Lenaerts, Anne J.,Massoudi, Lisa M.,Myers, Timothy G.,Myrick, Alissa,Nchinda, Aloysius T.,Njoroge, Mathew,Reddy, Virsinha,Robertson, Gregory T.,Singh, Vinayak,Sirgel, Frederick A.,Su, Qin,Van Helden, Paul D.,Müller, Rudolf
supporting information, p. 12790 - 12807 (2021/09/11)
Phenotypic whole cell high-throughput screening of a μ150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide 1 as a moderately active hit. Structure-activity
Synthesis of 1,5-diarylpyrazol-3-propanoic acids towards inhibition of cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4 formation
Erguen, Burcu Caliskan,Nunez, Maria Teresa,Labeaga, Luis,Ledo, Francisco,Darlington, Janice,Bain, Gretchen,Cakir, Bilge,Banoglu, Erden
experimental part, p. 497 - 505 (2011/05/09)
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.
