| Literature DB >> 8234177 |
M E Brewster1, E Pop, A J Braunstein, A C Pop, P Druzgala, A Dinculescu, W Anderson, A Elkoussi, N Bodor.
Abstract
Enhanced brain delivery of zidovudine (AZT) has been demonstrated using a redox-based chemical delivery system (CDS). Optimization of the prototype AZT-CDS (5'-[(1-methyl-1,4-dihydropyridin-3-yl)carbonyl]-3'-azido-3'-deoxy thymidine ) was investigated by manipulation of the N-methyl group present on the dihydronicotinate portion of the molecule and examining the release of AZT in vivo in a rat model. Of the five compounds examined, all produced higher brain levels and lower blood levels of AZT than did AZT itself. In comparing the novel AZT-CDS analogues to the N-methyl benchmark, the N-propyl system proved to be the most efficient of the compounds tested.Entities:
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Year: 1993 PMID： 8234177 DOI： 10.1023/a:1018986217181
Source DB: PubMed Journal: Pharm Res ISSN： 0724-8741 Impact factor: 4.200