molecules of the month


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

Structure of MGS0274, a potent and selective agonist of mGlu2 and mGlu3 receptors
1 min read

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).

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