| Literature DB >> 25468035 |
Yuanyuan Cao1, Yu Zhang2, Shaotong Wu2, Quanzhi Yang2, Xuefeng Sun2, Jianxiong Zhao2, Fen Pei2, Ying Guo2, Chao Tian2, Zhili Zhang2, Haining Wang3, Liying Ma3, Junyi Liu4, Xiaowei Wang5.
Abstract
A novel 2-pyridinone scaffold was rationally designed and synthesized based on the active anti-HIV agent 1 (LAM-trans) via an efficient method. The biological results revealed that some target compounds inhibited HIV-1 reverse transcriptase in the lower micromolar concentration range (IC50 0.089-0.68 μm). Notably, the most promising compound 25b exhibited extremely potent inhibitory activity against HIV-1 replication with an EC50 value of 0.0563 μM and the viral selectivity index amounted to 3466.8. Molecular modeling studies were performed, and some SARs were rationalized.Entities:
Keywords: HIV-1; NNRTIs; Pyridinone analogues
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Year: 2014 PMID： 25468035 DOI： 10.1016/j.bmc.2014.11.012
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641