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  • Title: Synthesis and evaluation of atorvastatin esters as prodrugs metabolically activated by human carboxylesterases.
    Author: Mizoi K, Takahashi M, Haba M, Hosokawa M.
    Journal: Bioorg Med Chem Lett; 2016 Feb 01; 26(3):921-923. PubMed ID: 26750256.
    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.
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