866638-72-4Relevant articles and documents
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)
Axford, Laura,Cohick, Evan,Dales, Natalie,Deng, Lin,Hamann, Lawrence G.,Harrison, Tyler J.,Hollis-Symynkywicz, Micah,Kecman, Sam,Lee, Lac,Loi, Sally,Marcinkeviciene, Jovita,Marro, Martin L.,Papillon, Julien P. N.,Patnaik, Anup,Patterson, Andrew W.,Regard, Jean B.,Ren, Xianglin
, (2020)
Myeloperoxidase (MPO) activity and subsequent generation of hypochlorous acid has been associated with the killing of host-invading microorganisms (e.g. bacteria, viruses, and fungi). However, during oxidative stress, high MPO activity can damage host tissue and is linked to several chronic inflammatory conditions. Herein, we describe the development of a novel biaryl, indole-pyrazole series of irreversible mechanism-based inhibitors of MPO. Derived from an indole-containing high-throughput screen hit, optimization efforts resulted in potent and selective 6-substituted indoles with good oral bioavailability and in vivo activity.
NOVEL IMIDAZOPYRAZINE DERIVATIVES
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Page/Page column 51; 197-198, (2021/12/31)
The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein Rx and R3 to R5 are as described herein (formula (I)) or pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Paragraph 1301, (2015/02/18)
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
