oral brain penetrant _-secretase modulator
oral reduction of CSF A_42 in model
rational design from literature starting point
J. Med. Chem., Aug. 13, 2020
Merck & Co., Kenilworth, NJ
“compound 20”
1 min read
“compound 20” is a gamma-secretase modulator (GSM) with an interesting, uncommon oxadiazine scaffold. Like many hot areas in drug discovery, the GSM area for Alzheimer’s has led to many creative chemical scaffolds. It’s always interesting to see how these new scaffolds behave. This compound demonstrates surprisingly low clearance, high bioavailability in rodents, and sufficient brain penetration to observe desired PD in vivo.
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