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The Pharmaceutical Society of Korea (대한약학회)
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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)
  • Published : 2006.11.30
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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

References

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