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

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

journal_name

Bioorg Med Chem

authors

Zhan P,Liu X,Fang Z,Pannecouque C,De Clercq E

doi

10.1016/j.bmc.2009.07.027

subject

Has Abstract

pub_date

2009-09-01 00:00:00

pages

6374-9

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00684-1

journal_volume

17

pub_type

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