Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
Regular Articles
Synthesis and Antiviral Activity of Phthiobuzone Analogues
Ya-Jun YangJing-Hua ZhaoXian-Dao PanPei-Cheng Zhang
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2010 Volume 58 Issue 2 Pages 208-211


A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4′,4″ position, show more potent antiviral activity than phthiobuzone against herpes simplex virus 1 (IC50=8.56 and 2.85 μg/ml, respectively) and herpes simplex virus 2 (IC50=1.75 and 4.11 μg/ml, respectively). Compounds 9c and 9d with a propylene linker between the phthalimide and bisthiosemicarbazone moieties display similar antiviral potency against herpes simplex virus 1 (IC50=2.85 and 4.11 μg/ml, respectively).

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© 2010 The Pharmaceutical Society of Japan
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