Introduction of a cyano group at the 2-position of an (R,S)-3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) derivative of thymine elicits selective anti-HBV activity.
RSC Med Chem
; 12(5): 804-808, 2021 May 26.
Article
em En
| MEDLINE
| ID: mdl-34124679
ABSTRACT
The substantial impact of acyclic nucleoside phosphonates (ANPs) on human medicine encourages the synthesis of new ANP analogues with a potentially differentiated antiviral spectrum. Herein, we demonstrate the functionalization of the 2-position of the (R,S)-3-hydroxy-2-(phosphonomethoxy)propyl side-chain of an inactive ANP with a polar cyano group to generate a thymine analogue with selective inhibition of hepatitis B virus (HBV) replication (SI > 302; EC50 = 0.33 µM), without significant antiretroviral activity. These findings suggest new strategies to synthesize unique ANPs with a targeted antiviral profile.
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01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
RSC Med Chem
Ano de publicação:
2021
Tipo de documento:
Article