| Title | Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs |
| Authors | Cao, Yuanyuan Zhang, Yu Wu, Shaotong Yang, Quanzhi Sun, Xuefeng Zhao, Jianxiong Pei, Fen Guo, Ying Tian, Chao Zhang, Zhili Wang, Haining Ma, Liying Liu, Junyi Wang, Xiaowei |
| Affiliation | Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China. Hubei Univ Med, Taihe Hosp, Shiyan 442000, Hubei, Peoples R China. Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China. Chinese Ctr Dis Control & Prevent, State Key Lab Infect Dis Prevent & Control, Natl Ctr AIDS STD Control & Prevent NCAIDS, Beijing 102206, Peoples R China. |
| Keywords | Pyridinone analogues HIV-1 NNRTIs REVERSE-TRANSCRIPTASE INHIBITORS DRUG-RESISTANCE DERIVATIVES DESIGN STRAINS SERIES |
| Issue Date | 2015 |
| Publisher | 生物有机化学与医药化学 |
| Citation | BIOORGANIC & MEDICINAL CHEMISTRY.2015,23,(1),149-159. |
| 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 mu m). Notably, the most promising compound 25b exhibited extremely potent inhibitory activity against HIV-1 replication with an EC50 value of 0.0563 mu M and the viral selectivity index amounted to 3466.8. Molecular modeling studies were performed, and some SARs were rationalized. (C) 2014 Elsevier Ltd. All rights reserved. |
| URI | http://hdl.handle.net/20.500.11897/156295 |
| ISSN | 0968-0896 |
| DOI | 10.1016/j.bmc.2014.11.012 |
| Indexed | SCI(E) PubMed |
| Appears in Collections: | 药学院 天然药物与仿生药物国家重点实验室 |
