合成膦酸酯3-邻苯二甲酰亚胺酯作为前药，用于膦酸酯的潜在细胞内递送。

Synthesis of phosphonate 3-phthalidyl esters as prodrugs for potential intracellular delivery of phosphonates.

作者信息

Dang Q, Brown B S, van Poelje P D, Colby T J, Erion M D

机构信息

Department of Medicinal Chemistry, Metabasis Therapeutics, Inc., San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1505-10. doi: 10.1016/s0960-894x(99)00239-5.

DOI:10.1016/s0960-894x(99)00239-5

PMID:10386925

Abstract

A new prodrug approach for intracellular delivery of phosphonates was developed via the synthesis of 3-phthalidyl esters of 1-naphthalenemethylphosphonate. This approach is advantageous over the traditional acyloxymethyl phosphonate prodrugs, because these prodrugs do not generate formaldehyde and have improved plasma half-lives.

摘要

通过合成1-萘甲基膦酸酯的3-邻苯二甲酰亚胺酯，开发了一种用于膦酸盐细胞内递送的新前药方法。这种方法优于传统的酰氧基甲基膦酸酯前药，因为这些前药不会产生甲醛，并且具有更长的血浆半衰期。