5 ',5 '-Phosphodiesters and esterase labile triesters of 2 '-C-methylribonucleosides
Research output: Contribution to journal › Article › Scientific › peer-review
|Number of pages||18|
|Publication status||Published - 2012|
|Publication type||A1 Journal article-refereed|
Bis(2'-C-methyladenosin-5'-yl) (11), bis(2'-C-methylguanosin-5'-yl) (13), bis(2'-C-methyluridin-5'-yl) (15) and 2'-C-methylguanosin-5'-yl 2'-C-methyluridin-5'-yl (16) phosphodiesters have been prepared as pro-drug candidates for the respective 2'-C-methylribonucleoside 5'-monophosphates, expectedly exhibiting antiviral activity against Hepatitis C virus. Additionally, the bis(2'-C-methyladenosine) diester has been converted to 3-acetyloxymethoxy-2,2-bis(ethoxycarbonyl)propyl (19) or pivaloyloxymethyl (20) triester. The underlying idea is that the 5',5'-phosphodiester is first released by intracellular carboxyesterases and subsequently cleaved to nucleoside and nucleoside 5'-monophosphate by phosphodiesterases.
- Pro-drug, antiviral, nucleotide, phosphoester, synthesis, CHRONIC HEPATITIS-C