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Bioorg Med Chem ; 6(9): 1481-9, 1998 Sep.
Article in English | MEDLINE | ID: mdl-9801819

ABSTRACT

This paper describes the new synthesis and evaluation of some morpholino- and pyrrolidinosphingolipids and mimics as inhibitors of glucosylceramide synthase. It was found that the pyrrolidino derivatives are generally more active than the morpholino derivatives and the best one was shown to be a nanomolar inhibitor.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Glucosyltransferases/antagonists & inhibitors , Sphingolipids/chemical synthesis , Sphingolipids/pharmacology , Drug Evaluation , Enzyme Inhibitors/chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Morpholines/chemistry , Pyrrolidines/chemistry , Spectrometry, Mass, Fast Atom Bombardment , Sphingolipids/chemistry
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