Garcia-Barrantes, Pedro M.; Cho, Hyekyung P.; Blobaum, Anna L.; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W. published the artcile< Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs>, SDS of cas: 337536-14-8, the main research area is VU0486321 analog preparation mGluR1 pos allosteric modulator pharmacokinetics schizophrenia; Metabotropic glutamate receptor; Positive allosteric modulator (PAM); Schizophrenia; Structure–activity relationship (SAR); mGlu(1).
This Letter describes the further lead optimization of the VU0486321 series of mGlu1 pos. allosteric modulators (PAMs), focused on addressing the recurrent issue of plasma instability of the phthalimide moiety. Here, the authors evaluated a number of phthalimide bioisosteres, and ultimately identified isoindolinones as the ideal replacement that effectively address plasma instability, while maintaining acceptable mGlu1 PAM potency, DMPK profile, CNS penetration and mGluR selectivity.
Bioorganic & Medicinal Chemistry Letters published new progress about Antipsychotics. 337536-14-8 belongs to class bromides-buliding-blocks, and the molecular formula is C9H8Br2O2, SDS of cas: 337536-14-8.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary