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Synthesis of Dimeric Trifluoromethoxyacridine‐derived Pathogen‐inactivating Nucleic Acid Intercalators
Author(s) -
Csuk René,
Raschke Christian,
Göthe Gunnar,
Reißmann Stefan
Publication year - 2004
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200400907
Subject(s) - chemistry , conjugate , nucleic acid , acridine , combinatorial chemistry , intercalation (chemistry) , stereochemistry , oligonucleotide , molecule , proflavine , biochemistry , dna , organic chemistry , mathematical analysis , mathematics
A series of antiviral active compounds consisting of an intercalating acridine‐derived part, a spacer region and a reactive EDTA‐derived conjugate was synthesized in an easy sequence. Thus, suitably mono‐protected 1, ω‐alkyldiamines gave, upon reaction with 9‐chloro‐2‐trifluoromethoxyacridine, followed by deprotection and reaction with EDTA dianhydride, the target molecules. Incorporation of their Fe(II) complexes in the presence of ascorbate gave a reduction of the phage titer of MS2 phages by several logarithmic decades.