Synthesis And Anti-Hiv Activity Of Novel 2,4-Disubstituted-7-Methyl-1,1,3-Trioxo-2h,4h-Pyrazolo[4,5-E][1,2,4] Thiadiazine Derivatives

DRUG DISCOVERIES AND THERAPEUTICS(2011)

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摘要
A series of novel 2,4-disubstituted-7-methyl-1,1,3-trioxo-2H,4H-pyrazolo[4,5-e] [1,2,4] thiadiazines (PTDs) was prepared starting from a ring of pyrazolo[4,5-e][1,2,4] thiadiazine nuclei with two different alkyl halides obtained by a facile one-pot reaction. The structures of all synthesized compounds were confirmed by H-1- and C-13-NMR, infrared spectra (IR), and mass spectra (MS) spectroscopic analysis. Anti-HIV activity was evaluated and none of the compounds were found to inhibit HIV replication in human T-lymphocyte (MT-4) cell culture.
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关键词
HIV, pyrazolo[4,5-e][1,2,4] thiadiazine, heterocycle, synthesis
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