Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound

Cyrille Tomassi; Van Nhien Albert Nguyen; José Marco-Contelles; Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Elena Soriano; Denis Postel

doi:10.1016/j.bmcl.2008.03.010

Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2277-81. doi: 10.1016/j.bmcl.2008.03.010. Epub 2008 Mar 7.

Authors

Cyrille Tomassi¹, Van Nhien Albert Nguyen, José Marco-Contelles, Jan Balzarini, Christophe Pannecouque, Erik De Clercq, Elena Soriano, Denis Postel

Affiliation

¹ Laboratoire des Glucides (UMR6219), Université de Picardie Jules Verne, 33 rue Saint Leu, 80039 Amiens, France.

PMID: 18353641
DOI: 10.1016/j.bmcl.2008.03.010

Abstract

The synthesis and the biological evaluation of the anti-HIV-1 activity of TSAO-Boc(3)T (8) are described. The computational analysis showed that the N-3 Boc group promotes new interactions in the binding site of the enzyme leading to a good inhibitory activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-HIV Agents / chemical synthesis
Anti-HIV Agents / pharmacology*
Binding Sites
Cell Line
HIV-1 / drug effects*
HIV-2 / drug effects*
Models, Chemical
Reverse Transcriptase Inhibitors / chemical synthesis
Reverse Transcriptase Inhibitors / pharmacology*
Spiro Compounds / chemistry*
Structure-Activity Relationship
Virus Replication / drug effects*

Substances

Anti-HIV Agents
Reverse Transcriptase Inhibitors
Spiro Compounds