Synthesis of α‐Methyldopa Prodrugs Containing Dipeptide Moieties as Tools for Intestinal Delivery

Hui‐Po ‐P Wang, Chih‐Yuan ‐Y Cheng, Jin‐Ran ‐R Ma, Jia‐Shuai ‐S Lee

研究成果: 雜誌貢獻文章同行評審

3 引文 斯高帕斯(Scopus)

摘要

Dipeptides containing D‐phenylglycine or D‐p‐hydroxyphenylglycine were attached onto the antihypertensive agent α‐methyldopa to form prodrugs 1a, 1b and 1c. The nonessential amino acids were introduced into the prodrug molecules as tools of chemical delivery to improve the intestinal absorption of the parent drug. Preliminary tests revealed that the prodrugs were stable in phosphate buffer solutions at pH 7.4 (t1/2 > 10 h). These compounds also demonstrated satisfactory stability toward enzymatic degradation in a mucosa preparation isolated from rat intestine, indicating that they might be feasibly formulated as an oral prodrug of α‐methyldopa.

原文英語
頁(從 - 到)561-567
頁數7
期刊Journal of the Chinese Chemical Society
42
發行號3
DOIs
出版狀態已發佈 - 1995
對外發佈

ASJC Scopus subject areas

  • 化學 (全部)

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