Optimization of the Antiviral Potency and Lipophilicity of Halogenated 2,6-Diarylpyridinamines as a Novel Class of HIV-1 NNRTIS
- Wu, Zhi Yuan
- Liu, Na
- Qin, Bingjie
- Huang, Li
- Yu, Fei
- Qian, Keduo
- Morris-Natschke, Susan L.
- Jiang, Shibo
- Chen, Chin Ho
- Lee, Kuo Hsiung
- Xie, Lan
Publication date
January 2014
DOIAbstract
Nineteen new halogenated diarylpyridinamine (DAPA) analogues (6a-n and 8a-e) modified on the phenoxy C-ring were synthesized and evaluated for anti-HIV activity and certain drug-like properties. Ten compounds showed high anti-HIV activity (EC50 0.3, LLE >5, LELP <10). With balanced potency and drug-like properties, 8c merits further development as an anti-HIV drug candidate