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Facile Synthesis of the CERT Inhibitor HPA‐12 and Some Novel Derivatives
Author(s) -
Saied Essa M.,
Diederich Stephanie,
Arenz Christoph
Publication year - 2014
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201402241
Subject(s) - sphingomyelin , ceramide , chemistry , golgi apparatus , membrane , combinatorial chemistry , biochemistry , cell , apoptosis
HPA‐12 is an inhibitor of CERT‐mediated non‐vesicular transport of ceramide from the ER membranes to the Golgi apparatus. The inhibitor effectively blocks the synthesis of the membrane lipid sphingomyelin and may represent a novel drug prototype. Previous syntheses relied on non‐commercial catalysts or specialized chemistries. Here we present a straightforward and effective method to synthesize HPA‐12 from commercially available protected L ‐serinol in four steps. Some new analogues were synthesized and evaluated for their CERT‐binding activity.