Citation: Xin Yong Liu, Ren Zhang Yan, Nian Gen Chen, Wen Fang Xu. Regioselective synthesis and anti-HIV activity of the novel 2-and 4-substituted pyrazolo[4,5-e] [1,2,4]thiadiazines[J]. Chinese Chemical Letters, ;2007, 18(2): 137-140. doi: 10.1016/j.cclet.2006.12.006 shu

Regioselective synthesis and anti-HIV activity of the novel 2-and 4-substituted pyrazolo[4,5-e] [1,2,4]thiadiazines

Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China

Received Date: 12 July 2006

Fund Project: The financial supports of this work by the National Natural Science Foundation of China (No. 30371686),Ministry of Science and Technology of China,for the key project of international cooperation (2003DF000033) and NSF Shandong Province (Y2003C11),are gratefully acknowledged. We also thank State New Drug Screening Center of Shanghai,for assistance with the HIV-1 RT assay.

The new regioisomer 7-methyl-pyrazolo[4,5-e] [1,2,4]thiadiazine nucleus (5) was synthesized, and its novel mono-N₂-or N₄-substituted pyrazolo[4,5-e] [1,2,4]thiadiazines (6, 7) were regioselectively prepared by deprotonation of NN₂ or/and N₄ atoms with different molar ratio of NaH and alkyl halides. Anti-HIV-1 screening tests showed some compounds to be potent as HIV-1 nonnucleoside reverse transcriptase inhibitors (HIV-1 NNRTIs).
- Pyrazolo[4,5-e][1,2,4]thiadiazine,
- Regioselectivity,
- Synthesis,
- HIV-1 NNRTIs
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