911307-33-0Relevant academic research and scientific papers
Synthesis and anti-HIV activity evaluation of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo-[4,5-e][1,2]thiadiazines
Liu, Xin-Yong,Yan, Ren-Zhang,Wang, Yan,Zhan, Peng,De Clercq, Erik,Pannecouque, Christophe,Witvrouw, Myriam,Molina, Maria Teresa,Vega, Salvador
experimental part, p. 216 - 222 (2009/04/03)
A series of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro- pyrazolo[4,5-e] [1,2,4]thiadiazines (PTDs) was synthesized, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activities by inhibition of HIV-induced cytopathogenicity in MT-4 cell culture. The results showed that some compounds exhibited inhibitory activity specifically against HIV-2 replication. The most active HIV-2 inhibitor was compound 7i (R 1 = benzyl, R2 = 4-t-butyl-benzyl) with an EC50 value of 18.7 μM and SI=15, which may provide a useful lead for further molecular optimization.
