2. Academic Validation
  3. First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication

First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication

  • J Med Chem. 2005 Jun 30;48(13):4276-84. doi: 10.1021/jm050091g.
Albert Nguyen Van Nhien 1,  Cyrille Tomassi,  Christophe Len,  José Luis Marco-Contelles,  Jan Balzarini,  Christophe Pannecouque,  Erik De Clercq,  Denis Postel
Affiliations

Affiliation

  • 1 Laboratoire des Glucides (FRE 2779), Faculté des Sciences, Université de Picardie Jules Verne, 33 rue Saint Leu, 80039 Amiens, France.
PMID: 15974581 DOI: 10.1021/jm050091g
Abstract

Aza TSAO-T derivatives bearing a dihydroisothiazole dioxide ring instead of an oxathiole dioxide ring at the C-3' position on the sugar moiety were prepared. We have synthesized four families of compounds depending on substitution at both N-3 and N-2' '. Biological evaluation showed that these compounds are HIV-1(III(B))-specific and potent Reverse Transcriptase inhibitors with EC(50) values between 0.13 and 3.5 microM in Cell Culture.

Figures