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ID: ALA3751766

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of atorvastatin esters as prodrugs metabolically activated by human carboxylesterases.

Authors: Mizoi K, Takahashi M, Haba M, Hosokawa M.

Abstract: We synthesized 11 kinds of prodrug with an esterified carboxylic acid moiety of atorvastatin in moderate to high yields. We discovered that they underwent metabolic activation specifically by the human carboxylesterase 1 (CES1) isozyme. The results suggested that these ester compounds of atorvastatin have the potential to act as prodrugs in vivo.

CiteXplore: 26750256

DOI: 10.1016/j.bmcl.2015.12.069