STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRROLE AMIDINE ANTI-VIRAL ANTIBIOTICS .1. MODIFICATIONS OF THE ALKYLAMIDINE SIDE-CHAIN

被引:23
作者
BIALER, M
YAGEN, B
MECHOULAM, R
BECKER, Y
机构
[1] HEBREW UNIV JERUSALEM,SCH PHARM,DEPT NAT PROD,JERUSALEM 91000,ISRAEL
[2] HEBREW UNIV JERUSALEM,SCH MED,DEPT MOLEC VIROL,JERUSALEM 91000,ISRAEL
关键词
D O I
10.1021/jm00197a004
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Representatives of three types of side-chain analogues of distamycin A (1) were synthesized. These were tested for cytotoxicity, inhibition of herpes simplex virus (HSV) replication in cultured cells, effects on the synthesis of HSV DNA in isolated nuclei in vitro, as well as on DNA synthesis by purified HSV DNA polymerase. Distamycin A was the most active compound in all three antiviral tests, as well as the most toxic. However, several compounds, in particular the aromatic analogues 15 and 16, showed no toxicity under the experimental conditions used but were still very active in the three antiviral tests. © 1979, American Chemical Society. All rights reserved.
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页码:1296 / 1301
页数:6
相关论文
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