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- W3148321246 abstract "NAD+ is a crucial cellular factor that plays multifaceted roles in wide ranging biological processes. Low levels of NAD+ have been linked to numerous diseases including metabolic disorders, cardiovascular disease, neurodegeneration, and muscle wasting disorders. A novel strategy to boost NAD+ is to activate nicotinamide phosphoribosyltransferase (NAMPT), the putative rate-limiting step in the NAD+ salvage pathway. We previously showed that NAMPT activators increase NAD+ levels in vitro and in vivo. Herein we describe the optimization of our NAMPT activator prototype (SBI-0797812) leading to the identification of 1-(4-((4-chlorophenyl)sulfonyl)phenyl)-3-(oxazol-5-ylmethyl)urea (34) that showed far more potent NAMPT activation and improved oral bioavailability." @default.
- W3148321246 created "2021-04-13" @default.
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- W3148321246 date "2021-06-01" @default.
- W3148321246 modified "2023-10-16" @default.
- W3148321246 title "Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators" @default.
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- W3148321246 doi "https://doi.org/10.1016/j.bmcl.2021.128007" @default.
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