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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors.

Franck DuclosLynn M AbellDavid G HardenKristen PikeKimberly NowakGregory A LockeGerald J DukeXiaoqin LiuGayani FernandoScott A ShawBenjamin P VokitsNicholas R WurtzAndrew VietMeriah N ValenteSylwia StachuraPaul SlephJaved A KhanJi GaoAshok R DongreLei ZhaoRuth R WexlerDavid A GordonEllen K Kick
Published in: MedChemComm (2017)
Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to invading pathogens. Myeloperoxidase has been implicated in several chronic pathological diseases due to the chronic production of hypochlorous acid, as well as other reactive radical species. A high throughput screen and triaging protocol was developed to identify a reversible inhibitor of myeloperoxidase toward the potential treatment of chronic diseases such as atherosclerosis. The identification and characterization of a reversible myeloperoxidase inhibitor, 7-(benzyloxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine is described.
Keyphrases
  • high throughput
  • randomized controlled trial
  • living cells
  • cardiovascular disease
  • microbial community
  • type diabetes
  • single cell
  • risk assessment
  • drug induced
  • antimicrobial resistance
  • human health
  • single molecule