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Synthesis and Preliminary Antiviral Activities of Piperidine‐substituted Purines against HIV and Influenza A/H1N1 Infections
Author(s) -
Kang Dongwei,
Fang Zengjun,
Huang Boshi,
Zhang Lingzi,
Liu Huiqing,
Pannecouque Christophe,
Naesens Lieve,
De Clercq Erik,
Zhan Peng,
Liu Xinyong
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12520
Subject(s) - rimantadine , amantadine , potency , purine metabolism , purine , influenza a virus , virology , virus , chemistry , ribavirin , piperidine , pharmacology , stereochemistry , biology , in vitro , biochemistry , enzyme , hepatitis c virus
We have developed a series of N 2 ‐(1‐(substituted‐aryl)piperidin‐4‐yl)‐N 6 ‐mesityl‐9 H ‐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, FZJ 13 appeared to be the most notable one, which displayed anti‐ HIV ‐1 activity compared to 3 TC . Moreover, an unexpected finding was that FZJ 05 displayed significant potency against influenza A/H1N1 (strain A/ PR /8/34) in Madin–Darby canine kidney cells with EC 50 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.