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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
Author(s) -
Liu Xinyong,
Yan Renzhang,
Wang Yan,
Zhan Peng,
De Clercq Erik,
Pannecouque Christophe,
Witvrouw Myriam,
Molina Maria Teresa,
Vega Salvador
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700216
Subject(s) - chemistry , human immunodeficiency virus (hiv) , stereochemistry , lead compound , medicinal chemistry , in vitro , biochemistry , virology , biology
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 μM and SI=15, which may provide a useful lead for further molecular optimization.