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Synthesis and antiviral evaluation of novel N-6 substituted adenosine analogues
Authors:Youwu Hao  Gaohui Zhou  Wei Wu  Yang Zhang  Liming Tao  Jianhua Yao  Wenping Xu
Affiliation:1. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;2. Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China
Abstract:
A series of adenosine analogues were synthesized and their biological evaluation was tested against Coxsackie virus B3 (CVB3) and Herpes simplex virus type 1(HSV-1) in HEp-2 cells. The hydrophobic constant, acute toxicity, carcinogenicity and mutagenicity were calculated. Analogues with piperazine derivatives 8b showed promising activities against CVB3 with a lower IC50value and higher selectivity index, their efficacy was better than that of the commercialized medicine, Ribavirin. These described adenosine analogues exhibit potent antiviral activities against several viruses, and offer new leads for further development.
Keywords:Adenosine analogues  Antiviral activities  Coxsackie virus B3  Herpes simplex virus type 1  Higher selectivity index
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