1352804-13-7Relevant academic research and scientific papers
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors
Liu, Xin,Liu, Xinyong,Chen, Xuwang,Zhan, Peng,Cheng, Ziheng,Meng, Caicai,Shao, Siyuan,Pannecouque, Christophe,De Clercq, Erik
, p. 3856 - 3864 (2012/08/13)
A novel series of piperidine-linked amino-triazine derivatives were designed, synthesized and evaluated for in vitro anti-HIV activity as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. Screening results indicated that most compounds showed excellent activity against wild-type HIV-1 with EC50 values in low nanomolar concentration range (especially compound 6b3, EC50 = 4.61 nM, SI = 5945) and high activity against K103N/Y181C resistant mutant strain of HIV-1 with EC50 values in low micromolar concentration range. In addition, preliminary structure-activity relationship and molecular modeling of these new analogs were detailed in this manuscript.
