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 (EC(50)=2.45 microM) similar to the prototype series of sulfanyltriazoles. None of the compounds were active against HIV-2 replication.
Zhan
Peng
P
Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012 , PR China.
Liu
Xinyong
X
Fang
Zengjun
Z
Pannecouque
Christophe
C
De Clercq
Erik
E
D000083:Acetanilides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects
C545033:1,2,3-selenadiazole thioacetanilide; D000083:Acetanilides; D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; C039632:thioacetanilide