کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363980 | 981525 | 2009 | 4 صفحه PDF | دانلود رایگان |
A novel approach to synthesize chitosan–O-isopropyl-5′-O-d4T monophosphate conjugate was developed. Chitosan-d4T monophosphate prodrug with a phosphoramidate linkage was efficiently synthesized through Atherton-Todd reaction. In vitro drug release studies in pH 1.1 and 7.4 indicated that chitosan–O-isopropyl-5′-O-d4T monophosphate conjugate prefers to release the d4T 5′-(O-isopropyl)monophosphate than free d4T for a prolonged period. The results suggested that chitosan–O-isopropyl-5′-O-d4T monophosphate conjugate may be used as a sustained polymeric prodrug for improving therapy efficacy and reducing side effects in antiretroviral treatment.
This work describes the novel synthesis of chitosan–O-isopropyl-5′-O-d4T monophosphate conjugate, allowing a sustained release of d4T 5′-(O-isopropyl)monophosphate for antiretroviral treatment.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 9, 1 May 2009, Pages 2566–2569