| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1359366 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
A small library of amino acid ester prodrugs of 6-β-naltrexol (NTXOL, 1) was prepared in order to investigate the candidacy of these prodrugs for microneedle-enhanced transdermal delivery. Six amino acid ester prodrugs were synthesized (6a–f). 6b, 6d, and 6e were stable enough at skin pH (pH 5.0) to move forward to studies in 50% human plasma. The lead compound (6e) exhibited the most rapid bioconversion to NTXOL in human plasma (t1/2 = 2.2 ± 0.1 h).
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Joshua A. Eldridge, Mikolaj Milewski, Audra L. Stinchcomb, Peter A. Crooks,