Synthesis and pre-clinical studies of new amino-acid ester thiazolide prodrugs

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• 作者：Andrew V. Stachulski^a ; ^{stachuls@liv.ac.uk} ; Karl Swift^b ; Mark Cooper^b ; Stephen Reynolds^b ; Daniel Norton^c ; Steven D. Slonecker^c ; Jean-Franç ; ois Rossignol^d
• 关键词：Antiviral agents ; Prodrugs ; Chemical synthesis ; Stability ; Biodisposition ; Oral absorption ; Pharmacology ; Toxicology
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：154-159
• 全文大小：446 K
• 卷排序：126

文摘

An effective phenolic prodrug for the antiviral agent tizoxanide and a 5-Cl analogue is described. These derivatives employ the amino-acid L-tertiary-leucine. The stability of this prodrug significantly exceeds that of the Val or Ile analogues. Good blood levels are obtainable by oral or IV administration. The compounds show a good safety profile.