SYNTHESIS OF PHILANTHOTOXIN ANALOGS WITH A BRANCHED POLYAMINE MOIETY

被引:24
作者
KALIVRETENOS, AG [1 ]
NAKANISHI, K [1 ]
机构
[1] COLUMBIA UNIV, DEPT CHEM, NEW YORK, NY 10027 USA
关键词
D O I
10.1021/jo00076a017
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Philanthotoxin (PhTX-433), a potent noncompetitive inhibitor of the L-glutamate receptors and the nicotinic acetylcholine receptors of vertebrates and invertebrates, has a butyryl-tyrosyl-thermo-spermine structure. Several synthetic analogs of PhTX with hydrophobic alkyl branches in the polyamine chain exhibit 6- to 10-fold enhanced activities to various receptors. Because the branched analogs exhibit such unique activities and because of their importance in tertiary structural studies of ligand/receptor binding, methods for preparing branched PhTX analogs, including photolabile analogs, are presented.
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页码:6596 / 6608
页数:13
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