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Synthesis and biological evaluation of novel 2-arylalkylthio-5-iodine-6-substituted-benzyl-pyrimidine-4(3H)-ones as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. 2014
Liang Zhang, and
Xiaowan Tang, and
Yuanyuan Cao, and
Shaotong Wu, and
Yu Zhang, and
Jianxiong Zhao, and
Ying Guo, and
Chao Tian, and
Zhili Zhang, and
Junyi Liu, and
Xiaowei Wang
Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
A novel series of 2-arylalkylthio-5-iodine-6-substitutedbenzyl-pyrimidine-4(3H)-ones (S-DABOs) 8a-x had been synthesized via an efficient method. Their biological activity against HIV virus and RT assay were evaluated. Some compounds, especially 8h, 8l and 8n, displayed promising activity against HIV-1 RT with IC50 values in a range of 0.41 μM to 0.71 μM, which were much better than that of nevirapine. Molecular modeling studies revealed that the binding mode would be affected via forming an additional hydrogen bond by incorporating an oxygen atom on the C-2 side chain. The biological activity was in accordance with the docking results.
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