Isoform-selective modulators for metabotropic glutamate receptors and protein kinase C: Synthesis and biological evaluation

✍ Scribed by Ma Da-Wei

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: English
• Weight: 619 KB
• Volume: 16
• Category: Article
• ISSN: 0256-7660
• DOI: 10.1002/cjoc.19980160402

✦ Synopsis

The synthetic studies for some known modulators of metabotropic glutamate receptors (mGluRs) such M (S)-aM4CPG, (lS,BR)-ACPD, LCCG-I are described. Based on the structure of aM4CPG several new conformationally constrained analogues are design ed and synthesized. Among them APICA is a selective antagonist for group I1 mGluRs. Also, a new benzolactam-V8 analogue h found to have better isoform-selectivity for protein k i n e C family. Three different protocols for synthesizing benzolactam-VS analogues are developed to meet the requirement for delivering more ma-.logues to test.