Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

This letter describes the further lead optimization of the VU0486321 series of mGlu(1) positive allosteric modulators (PAMs), focused on addressing the recurrent issue of plasma instability of the phthalimide moiety. Here, we evaluated a number of phthalimide bioisosteres, and ultimately identified...

Descripción completa

Guardado en:
Detalles Bibliográficos
Publicado en:Bioorg Med Chem Lett
Autores principales: Garcia-Barrantes, Pedro M., Cho, Hyekyung P., Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Lenguaje:Inglês
Publicado: 2016
Materias:
Article
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC4823774/
https://ncbi.nlm.nih.gov/pubmed/26988302
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.03.031
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!

Ejemplares similares