oral prodrug of mGlu2/3 receptor agonist
in development for schizophrenia
from derivatization of active molecule
Eur. J. Med. Chem., Jul. 5, 2020
Taisho Pharmaceutical, Saitama, JP
MGS0274 is a prodrug of an mGlu2/3 receptor agonist with ca. 15x greater oral exposure than the parent. The ester is believed to be cleaved pre-systemically by liver carboxyesterases to release the innocuous byproducts acetaldehyde, CO2, and menthol. The parent is also an interesting looking molecule prepared in a few steps from cyclopentenone (ref. 9 in article).