期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 6, 页码 1860-1865出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.02.007
关键词
1,2,3-Triazole derivatives; Diazocompounds; Anti-HSV-1
资金
- FAPERJ
- CNPq
- UFF
- CAPES
- CNPq-PIBIC
In this work, a new series of arysulfonylhydrazine-1H-1,2,3-triazole derivatives were synthesized, and their ability to inhibit the in vitro replication of HSV-1 was evaluated. Among the 1,2, 3-triazole derivatives, 1-[(5 ''-methyl-1 ''-(4'''-fluorophenylamino)-1H-1,2,3-triazol-4 ''-yl) carbonyl]-2-(4'-meth- ylphenylsulfonyl)hydrazine and 1-[(5'-methyl-1'-(2 '',5 ''-dichlorophenylamino)-1H-1,2,3-triazol-4'-yl)carbonyl]-2-(phenylsulfonyl)hydrazine, with IC50 values of 1.30 and 1.26 mu M, respectively, displayed potent activity against HSV-1. Because these compounds have low cytotoxicity, their selectivity indices are high. Under the assay conditions, they have better performance than does the reference compound acyclovir. The structures of all of the compounds were confirmed by one-and two-dimensional NMR techniques (H-1, C-13-APT, COSY-H-1 x H-1 and HETCOR (1)J(CH)) and by elemental analysis. (C) 2011 Elsevier Ltd. All rights reserved.
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