The author of 《Phenyldihydropyrazolones as Novel Lead Compounds Against Trypanosoma cruzi》 were Sijm, Maarten; Siciliano de Araujo, Julianna; Kunz, Stefan; Schroeder, Susanne; Edink, Ewald; Orrling, Kristina M.; Matheeussen, An; van de Meer, Tiffany; Sadek, Payman; Custers, Hans; Cotillo, Ignacio; Martin, Julio J.; Siderius, Marco; Maes, Louis; Brown, David G.; de Nazare Correia Soeiro, Maria; Sterk, GeertJan; de Esch, Iwan J. P.; Leurs, Rob. And the article was published in ACS Omega in 2019. HPLC of Formula: 1692-25-7 The author mentioned the following in the article:
As over 6 million people are infected with Chagas disease and only limited therapeutic options are available, there is an urgent need for novel drugs. The involvement of cyclic nucleotide phosphodiesterases (PDE) in the life cycle and biol. fitness of a number of protozoan parasites has been described and several of these enzymes are thought to be viable drug targets. Within this context, a PDE-focused library was screened for its ability to affect the viability of Trypanosoma cruzi parasites. Previously reported human PDE4 inhibitor, 5-(3-(benzyloxy)-4-methoxyphenyl)-2-isopropyl-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one, was identified as a hit. Upon optimization on three positions of the phenylpyrazolone scaffold, 2-isopropyl-5-(4-methoxy-3-(pyridin-3-yl)phenyl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one (I) proved to be the most active compound against intracellular forms of T. cruzi (pIC50 = 6.4) with a 100-fold selectivity with respect to toxicity towards human MRC-5 cells. Evaluation on different life stages and clin. relevant T. cruzi strains revealed that the phenylpyrazolones are not active against the bloodstream form of the Y strain but show submicromolar activity against the intracellular form of the Y- and Tulahuen strains as well as against the nitro-drug resistant Colombiana strain. In vitro screening of phenylpyrazolones against TcrPDEB1, TcrPDEC and TcrCYP51 showed that there was a poor correlation between enzyme inhibition and the observed phenotypic effect. Amongst the most potent compounds both TcrCYP51 and non-TcrCYP51 inhibitors are identified, which were both equally able to inhibit T. cruzi in vitro. In addition to this study using Pyridin-3-ylboronic acid, there are many other studies that have used Pyridin-3-ylboronic acid(cas: 1692-25-7HPLC of Formula: 1692-25-7) was used in this study.
Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. HPLC of Formula: 1692-25-7