1. Academic Validation
  2. Synthesis and antiviral activity of new dimeric inhibitors against HIV-1

Synthesis and antiviral activity of new dimeric inhibitors against HIV-1

  • Bioorg Med Chem. 2008 Jan 1;16(1):511-7. doi: 10.1016/j.bmc.2007.09.015.
Krzysztof Danel 1 Louise M Larsen Erik B Pedersen Giuseppina Sanna Paolo La Colla Roberta Loddo
Affiliations

Affiliation

  • 1 Nucleic Acid Center, Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
Abstract

This paper describes the synthesis and the Antiviral activities of dimeric compounds derived from homo and asymmetric combinations of N-1 propynyloxymethyl analogues 1a,b of MKC-442, an N-1 4-iodobenzyloxymethyl analogue of TNK-651 5, potent contraceptive norgestrel and AZT. They were obtained by Sonogashira reaction, 'click' chemistry or Pd-catalyzed oxidative coupling. The iodo precursor 5 turned out as a potent compound against wild type and mutated HIV-1 virus. All dimeric compounds showed lower activity against HIV-1 than MKC-442, except the asymmetric dimer of AZT and 1a which showed an activity comparable to MKC-442.

Figures