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M9490729.TXT
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1994-09-24
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Document 0729
DOCN M9490729
TI Synthesis and antiviral activity of three pyrazole analogues of
distamycin A.
DT 9411
AU Ding L; Grehn L; De Clercq E; Andrei G; Snoeck R; Balzarini J; Fransson
B; Ragnarsson U; Department of Biochemistry, Uppsala University, Sweden.
SO Acta Chem Scand. 1994 Jun;48(6):498-505. Unique Identifier : AIDSLINE
MED/94338814
AB The synthesis of three new monopyrazole analogues of the antiviral
compound distamycin A is reported. Suitably protected
4-amino-1-methylpyrrole-2-carboxylic acid and
3-amino-1-methylpyrazole-5-carboxylic acid derivatives were chosen as
starting materials. The construction of the trimeric polyamide framework
was accomplished by assembly of the monomeric precursors under
condensing conditions by analogy with our previous methodology, although
with significant improvements in some pivotal steps. After
chromatographic purification and spectroscopic characterisation, the
analogues were assayed for antiviral activity. Compounds 7a-c inhibited
vaccinia virus at a concentration similar to or lower than distamycin A
and the related antibiotic netropsin. Analogues 7b and 7c exhibited an
antiviral effect comparable to those of distamycin A and netropsin
against HSV-1 and HSV-2, whereas their antiviral activity against
several other viruses including HIV-1 and HIV-2 was somewhat lower. The
cellular toxicity of 7a-c toward different host cell types proved to be
of similar magnitude or lower than those of distamycin A and netropsin.
DE Animal Antiviral Agents/*CHEMICAL SYNTHESIS/TOXICITY Cell Line
Comparative Study Distamycins/*CHEMICAL SYNTHESIS/TOXICITY Human
HIV-1/DRUG EFFECTS HIV-2/DRUG EFFECTS Indicators and Reagents
Intercalating Agents/CHEMICAL SYNTHESIS Mice Molecular Structure
Netropsin/TOXICITY Pyrazoles/*CHEMICAL SYNTHESIS/TOXICITY Support,
Non-U.S. Gov't Vaccinia Virus/DRUG EFFECTS Viruses/*DRUG EFFECTS
JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).