Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors

  • Bioorg Med Chem Lett. 2009 Jul 1;19(13):3615-8. doi: 10.1016/j.bmcl.2009.04.132.
Suvi Rajamaki  1 ,  Anna Innitzer ,  Chiara Falciani ,  Cristina Tintori ,  Frauke Christ ,  Myriam Witvrouw ,  Zeger Debyser ,  Silvio Massa ,  Maurizio Botta
Affiliations
  • 1. Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via A. De Gasperi 2, I-53100 Siena, Italy.
PMID: 19447621 DOI: 10.1016/j.bmcl.2009.04.132
Abstract

A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and cellular assays.