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

• 作 者: 马大为
• 机 构: Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,Shangha 200032,China
• 出 处: Chinese Journal of Chemistry
• 发表日期: 1998年04期
• 关键词: analogues glutamate selectivity synthesizing afford substituted catalyzed hydrog

The synthetic studies for some known modulators of metabotropic glutamate receptors (mGluRs) such as (S)-αM4CPG,(1S,3fi)-ACPD,L-CCG-I are described.Based on the structure of αM4CPG several new conformationally constrained analogues are design ed and synthesized.Among them APICA is a selective antagonist for group II mGluRs.Also,a new benzolactam-V8 analogue is found to have better isoform-selectivity for protein kinase C family.Three different protocols for synthesizing benzolactam-V8 analogues are developed to meet the requirement for delivering more analogues to test.

The synthetic studies for some known modulators of metabotropic glutamate receptors (mGluRs) such as (S) -αM4CPG, (1S, 3fi) -ACPD, L-CCG-I are described.Based on the structure of αM4CPG several new conformationally constrained analogues are design ed and synthesized. Amm them APICA is a selective antagonist for group II mGluRs.Also, a new benzolactam-V8 analogue is found to have better isoform-selectivity for protein kinase C family. Three different protocols for synthesizing benzolactam-V8 analogues are developed to meet the requirement for delivering more analogues to test.