(Z)- and (E)-2-(hydroxymethylcyclopropylidene)methylpurines and pyrimidines as antiviral agents
(Z)- and (E)-2-(hydroxymethylcyclopropylidene)methylpurines and pyrimidines as antiviral agents
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DOI：
10.1177/095632029800900406
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发表时间：
1998-07-01
影响因子：
--
通讯作者：
Zemlicka, J
中科院分区：
文献类型：
--
作者：
Qiu, YL;Ptak, RG;Zemlicka, J
Several Z- and E-methylenecyclopropane nucleoside analogues were synthesized and tested for antiviral activity in vitro against human and murine cytomegalovirus (HCMV, MCMV), Epstein-Barr virus (EBV), varicella tester vii us (VZV), hepatitis B virus (HBV), herpes simplex virus types 1 and 2 (HSV-1, HSV-2), human herpesvirus 6 (HHV-6) and human immunodeficiency virus type 1 (HIV-1). The Z-2-amino-6-cyclopropylaminopurine analogue was the most effective agent against HCMV (EC50 or EC90 0.4-2 mu M) followed by syncytol and the Z-2,6-diaminopurine analogues (EC50 or EC90 3.4-29 and 11-24 mu M, respectively). The latter compound was also a strong inhibitor of MCMV (EC50 0.6 mu M). Syncytol was the most potent against EBV (EC50 74 mu M in HSV-1 and HSV-2 assays. 2-Amino-6-cyclopropylaminopurine and 2,6-diaminopurine derivatives were effective against HBV (EC50 and 10 mu M, respectively), whereas none of the analogues inhibited HIV-1 at a higher virus load. Syncytol and the E isomer were equipotent against EBV in Daudi cells but the E isomer was much less effective in DNA hybridization assays. The E-2,6-diaminopurine analogue and E isomer of synthymol were devoid of antiviral activity.
