标题：Synthesis and Preliminary Antiviral Activities of Piperidine-substituted Purines against HIV and Influenza A/H1N1 Infections
作者：Kang, Dongwei; Fang, Zengjun; Huang, Boshi; Zhang, Lingzi; Liu, Huiqing; Pannecouque, Christophe; Naesens, Lieve; De Clercq, Erik; Zha 更多 作者机构：[Kang, Dongwei; Fang, Zengjun; Huang, Boshi; Zhang, Lingzi; Zhan, Peng; Liu, Xinyong] Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med Chem,Ke 更多
通讯作者地址：[Zhan, P]Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Dept Med Chem,Key Lab Chem Biol, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China.
来源：CHEMICAL BIOLOGY & DRUG DESIGN
关键词：bioactivity; heterocycle; HIV; influenza virus; NNRTIs;; structure-activity relationship; synthesis
摘要：We have developed a series of N-2-(1-(substituted-aryl)piperidin-4-yl)-N-6-mesityl-9H-purine-2,6-diamine derivatives as potent antiviral agents. Preliminary biological evaluation indicated that nearly half of them possessed remarkable HIV inhibitory potencies in cellular assays. In particular, FZJ13 appeared to be the most notable one, which displayed anti-HIV-1 activity compared to 3TC. Moreover, an unexpected finding was that FZJ05 displayed significant potency against influenza A/H1N1 (strain A/PR/8/34) in Madin-Darby canine kidney cells with EC50 values much lower than those of ribavirin, amantadine, and rimantadine. The results suggest that these novel purine derivatives have the potential to be further developed as new therapeutic agents against HIV-1 or influenza virus.