Effect of structure on antibiotic action of new 9-(ethylthio)acridines.
Six new 9-(ethylthio)acridine derivatives were examined for antibacterial and antifungal activities with 10 bacterial and 8 yeast strains. The only active compounds were 2- and 3-amino derivatives. The observed MICs (mg/L) for 2-amino-9-(ethylthio)acridine (possessing the highest biological activity) were 12 (P. mirabilis), 30 (B. subtillis), 60 (C. freundii), 90 (E. coli), 128 (E. vulneris) and 500 (S. marcescens and S. aureus). Both amino derivatives have also lowest half-wave potential (E1/2) and field Swain-Lupton constants (describing oxidoreduction behavior) what supports the importance of acridine ion formation in the mechanism of antimicrobial action.
Nesmĕrák
K
K
Department of Analytical Chemistry, Faculty of Science, Charles University, 128 43 Prague, Czechia.
Pospisek
M
M
Zikánová
B
B
Nĕmec
I
I
Barbe
J
J
Gabriel
J
J
D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D015003:Yeasts / Q000187:drug effects*
D000166:Acridines; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents