Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.

Yuan‐Zhen Xiong; Hairong Hu; Fen‐Er Chen; Jan Balzarini; Christophe Pannecouque; De Clercq Erik

Back

Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.

Article 2009 en

Authors

YX
Yuan‐Zhen Xiong
HH
Hairong Hu
FC
Fen‐Er Chen

Abstract

1 min read

Eight new diaryltriazine derivatives containing 4-allylamino and 4-azido substitutes guided by molecular docking have been designed and synthesized based on our previous work. The evaluation of HIV inhibitory activity demonstrated that all compounds were potent against HIV-1 replication. The most active compound 7c exhibited activity against HIV-1 (IC50 = 0.034 micromol x L(-1), SI = 6,475) and the double mutant strain (IC50 = 9.39 micromol x L(-1)) in the micromolar range, which was more potent than nevirapine.

Discussion(0)

No comments yet. Be the first to comment.

Related publications

Article2018

Discovery of potent <scp>HIV</scp>‐1 non‐nucleoside reverse transcriptase inhibitors by exploring the structure–activity relationship of solvent‐exposed regions I

Dongwei Kang, Zhao Wang, Meng Chen, Da Feng, Gaochan Wu, Zhongxia Zhou, Lanlan Jing, Xiaofang Zuo, Xiangyi Jiang, Dirk Daelemans, De Clercq Erik, Christophe Pannecouque, Peng Zhan, Xinyong Liu

Article2014

Synthesis and biological evaluation of new conformationally restricted S-DABO hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Hai-Qiu Wu, Christophe Pannecouque, Zihong Yan, Wenxue Chen, Qiuqin He, Fen‐Er Chen, Jan Balzarini, Dirk Daelemans, De Clercq Erik

Article2022

Identification of Boronate-Containing Diarylpyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

Da Feng, Hao Lin, Liyang Jiang, Zhao Wang, Yanying Sun, Zhongxia Zhou, De Clercq Erik, Christophe Pannecouque, Dongwei Kang, Peng Zhan, Xinyong Liu

Article2009

Non‐Nucleoside HIV‐1 Reverse Transcriptase Inhibitors. Part 13

Yuan‐Zhen Xiong, Fen‐Er Chen, Jan Balzarini, De Clercq Erik, Christophe Pannecouque

Article2013

Discovery of Piperidine‐Linked Pyridine Analogues as Potent Non‐nucleoside HIV‐1 Reverse Transcriptase Inhibitors

Xuwang Chen, Yuanyuan Li, Shufang Ding, Jan Balzarini, Christophe Pannecouque, De Clercq Erik, Huiqing Liu, Xinyong Liu