Bioorganic & Medicinal Chemistry 2009-09-01

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

Peng Zhan, Xinyong Liu, Zengjun Fang, Christophe Pannecouque, Erik De Clercq

文献索引：Bioorg. Med. Chem. 17(17) , 6374-9, (2009)

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摘要

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 (EC(50)=2.45 microM) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication.