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Isoform‐selective modulators for metabotropic glutamate receptors and protein kinase C: Synthesis and biological evaluation
Author(s) -
DaWei Ma
Publication year - 1998
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.19980160402
Subject(s) - chemistry , metabotropic glutamate receptor , metabotropic glutamate receptor 2 , metabotropic receptor , metabotropic glutamate receptor 1 , gene isoform , glutamate receptor , metabotropic glutamate receptor 5 , protein kinase c , metabotropic glutamate receptor 6 , biochemistry , receptor , pharmacology , neuroscience , kinase , gene , psychology , medicine
Abstract The synthetic studies for some known modulators of metabotropic glutamate receptors (mGluRs) such as (S)‐αM4CPG, (1 S ,3 R )‐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 kine C family. Three different protocols for synthesizing benzolactam‐VS analogues are developed to meet the requirement for delivering more analogues to test.