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1,2,3-Selenadiazole thioacetanilides: Synthesis and anti-HIV activity evaluation
Authors:Peng Zhan   Xinyong Liu   Zengjun Fang   Christophe Pannecouque  Erik De Clercq
Affiliation:aInstitute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012 , PR China;bRega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium
Abstract: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 μM) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication.
Keywords:HIV-1   AIDS   NNRTIs   Selenadiazole   Anti-HIV-1 activity
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