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 |
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| Authors: | Ren-Zhang Yan Xin-Yong Liu Wen-Fang Xu Christophe Pannecouque Myriam Witvrouw Erik De Clercq |
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| Institution: | (1) Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, 250012 Jinan, China;(2) Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium |
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| Abstract: | A novel series of 2-(m-Chlorobenzyl)-4-substituted-1, 1, 3-trioxo-2H,4H-pyrazolo4, 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 EC50 value of 45.6 μM, but none of the compounds exhibited inhibitory activity against HIV-2. |
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| Keywords: | Synthesis Pyrazolothiadiazines HIV-1 NNRTIs MT-4 cells |
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