Phosphate prodrugs of PD154075

Authors
Zhu, ZJ Chen, HG Goel, OP Chan, OH Stilgenbauer, LA Stewart, BH
Citation
Zj. Zhu et al., Phosphate prodrugs of PD154075, BIOORG MED, 10(10), 2000, pp. 1121-1124
Citations number
28
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1121 - 1124
Database
ISI
SICI code
0960-894X(20000515)10:10<1121:PPOP>2.0.ZU;2-1
Abstract
In the preparation of phosphate prodrugs of PD154075, several strategies of linking a phosphate group to the indole moiety were studied, A novel linke r, p-hydroxymethylbenzoyloxymethoxycarbonyl was discovered to provide the p hosphate prodrug of PD154075 (compound 9) with significantly increased aque ous solubility, sufficient stability in aqueous solution and good bio-recon version in vivo, (C) 2000 Elsevier Science Ltd. All rights reserved.