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- Title
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.
- Authors
Liang Zhang; Xiaowan Tang; Yuanyuan Cao; Shaotong Wu; Yu Zhang; Jianxiong Zhao; Ying Guo; Chao Tian; Zhili Zhang; Junyi Liu; Xiaowei Wang
- Abstract
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.
- Subjects
HIV infection genetics; AROMATIC compound synthesis; ALKYL compounds; IODINE compounds synthesis; REVERSE transcriptase structure
- Publication
Molecules, 2014, Vol 19, Issue 6, p7104
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules19067104