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Synthesis and Anti-HIV Evaluation of the Novel 2-(m-Chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines  

Yan, Ren-Zhang (Institute of Medicinal Chemistry, School of Pharmacy, Shandong University)
Liu, Xin-Yong (Institute of Medicinal Chemistry, School of Pharmacy, Shandong University)
Xu, Wen-Fang (Institute of Medicinal Chemistry, School of Pharmacy, Shandong University)
Pannecouque, Christophe (Rega Institute for Medical Research, Katholieke Universiteit Leuven)
Witvrouw, Myriam (Rega Institute for Medical Research, Katholieke Universiteit Leuven)
Clercq, Erik De (Rega Institute for Medical Research, Katholieke Universiteit Leuven)
Publication Information
Archives of Pharmacal Research / v.29, no.11, 2006 , pp. 957-962 More about this Journal
Abstract
A novel series of 2-(m-Chlorobenzyl)-4-substituted-1, 1, 3-trioxo-2H, 4H-pyrazolo[4, 5-e][1, 2, 4] thiadiazines (7a-k) were synthesized, and evaluated for their anti-HIV replication in MT-4 cell cultures. Compound (7a) showed activity against HIV-1-induced cytopathicity, with an $EC_{50}$ value of $45.6\;{\mu}M$, but none of the compounds exhibited inhibitory activity against HIV-2.
Keywords
Synthesis; Pyrazolothiadiazines; HIV-1; NNRTIs; MT-4 cells;
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