62805-37-2Relevant academic research and scientific papers
Potent Triazolopyridine Myeloperoxidase Inhibitors
Wurtz, Nicholas R.,Viet, Andrew,Shaw, Scott A.,Dilger, Andrew,Valente, Meriah N.,Khan, Javed A.,Jusuf, Sutjano,Narayanan, Rangaraj,Fernando, Gayani,Lo, Fred,Liu, Xiaoqin,Locke, Gregory A.,Kopcho, Lisa,Abell, Lynn M.,Sleph, Paul,Basso, Michael,Zhao, Lei,Wexler, Ruth R.,Duclos, Franck,Kick, Ellen K.
, p. 1175 - 1180 (2018)
Myeloperoxidase (MPO) generates reactive oxygen species that potentially contribute to many chronic inflammatory diseases. A recently reported triazolopyrimidine MPO inhibitor was optimized to improve acid stability and remove methyl guanine methyl transferase (MGMT) activity. Multiple synthetic routes were explored that allowed rapid optimization of a key benzyl ether side chain. Crystal structures of inhibitors bound to the MPO active site demonstrated alternate binding modes and guided rational design of MPO inhibitors. Thioether 36 showed significant inhibition of MPO activity in an acute mouse inflammation model after oral dosing.
TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE
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Paragraph 00127, (2017/03/21)
The present invention provides compounds of Formula (I): wherein A, Y and R1 are each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
TRIAZOLOPYRIDINE AND TRIAZOLOPYRIMIDINE INHIBITORS OF MYELOPEROXIDASE
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Paragraph 00203, (2016/06/01)
The present invention provides compounds of Formula (I): wherein A and R1 are each as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
