1,2,3-Selenadiazole thioacetanilides: Synthesis and anti-HIV activity evaluation

The development of new HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosteric principle, novel series of 1,2,3-selenadiazole thioacetanilide derivatives were designed, and synthesized using an original synthetic route, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activity in MT-4 cells. The results showed that only compound 7f possessed potent activity against HIV-1 replication (EC50 = 2.45 mu M) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved.