1352804-07-9Relevant academic research and scientific papers
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
Chen, Xuwang,Zhan, Peng,Pannecouque, Christophe,Balzarini, Jan,De Clercq, Erik,Liu, Xinyong
experimental part, p. 60 - 66 (2012/07/14)
A novel series of piperidine-substituted triazine derivatives have been synthesized and evaluated for anti-HIV activities in MT-4 cells. Most compounds displayed extremely promising activity against wild-type HIV-1 with EC 50 values in low nanomolar concentration, better than that of Nevirapine, Delavirdine, Zidovudine and Dideoxycitidine, and higher potency towards the resistant mutant strain K103N/Y181C than that of Nevirapine and Delavirdine. Selected compounds were also assayed against reverse transcriptase with lower IC50 values than that of Nevirapine. The structure-activity relationship (SAR) of these novel structural congeners was also discussed.
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
experimental part, 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.
