111869-50-2Relevant academic research and scientific papers
9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors
Rodrigues, Marili V.N.,Barbosa, Alexandre F.,Da Silva, Júlia F.,Dos Santos, Deborah A.,Vanzolini, Kenia L.,De Moraes, Marcela C.,Corrêa, Arlene G.,Cass, Quezia B.
, p. 226 - 231 (2016)
A novel potent xanthine oxidase inhibitor, 3-nitrobenzoyl 9-deazaguanine (LSPN451), was selected from a series of 10 synthetic derivatives. The enzymatic assays were carried out using an on-flow bidimensional liquid chromatography (2D LC) system, which allowed the screening the measurement of the kinetic inhibition constant and the characterization of the inhibition mode. This compound showed a non-competitive inhibition mechanism with more affinity for the enzyme-substrate complex than for the free enzyme, and inhibition constant of 55.1 ± 9.80 nM, about thirty times more potent than allopurinol. Further details of synthesis and enzymatic studies are presented herein.
