Drug Discov Ther. 2011;5(6):279-285. (DOI: 10.5582/ddt.2011.v5.6.279)

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.

Zhan P, Yan RZ, Liu XY, Pannecouque C, Witvrouw M, De Clercq E, Molina MT, Vega S


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 1H- and 13C-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.

KEYWORDS: HIV, pyrazolo[4,5-e][1,2,4]thiadiazine, heterocycle, synthesis

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