Title: 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
Authors: Liu, Xin-Yong ×
Yan, Ren-Zhang
Wang, Yan
Zhan, Peng
De Clercq, Erik
Pannecouque, Christophe
Witvrouw, Myriam
Molina, Maria Teresa
Vega, Salvador #
Issue Date: Apr-2008
Series Title: Archiv der Pharmazie vol:341 issue:4 pages:216-222
Abstract: 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, R(2) = 4-t-butyl-benzyl) with an EC(50 )value of 18.7 muM and SI=15, which may provide a useful lead for further molecular optimization.
ISSN: 0365-6233
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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