Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA (CROSBI ID 251728)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Bistrović, Andrea ; Krstulović, Luka ; Stolić, Ivana ; Drenjančević, Domagoj ; Talapko, Jasminka ; Taylor, Martin C. ; Kelly, John M. ; Bajić, Miroslav ; Raić-Malić, Silvana
engleski
Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA
Amidinobenzimidazole derivatives connected to 1- aryl-substituted 1, 2, 3-triazole through phenoxymethylene linkers 7a–7e, 8a–8e and 9a–9e were designed and synthesized with the aim of evaluating their anti-bacterial and anti- trypanosomal activities and DNA/RNA binding affinity. Results from anti-bacterial evaluations of antibiotic resistant pathogenic bacteria revealed that both o-chlorophenyl-1, 2, 3-triazole and N-isopropylamidine moieties in 8c led to strong inhibitory activity against resistant Gram- positive bacteria, particularly the MRSA strain. Furthermore, the non-substituted amidine and phenyl ring in 7a induced a marked anti-bacterial effect, with potency against ESBL-producing Gram- negative E. coli better than those of the antibiotics ceftazidime and ciprofloxacin. UV-Vis and CD spectroscopy, as well as thermal denaturation assays, indicated that compounds 7a and 8c showed also binding affinities toward ctDNA Anti-trypanosomal evaluations showed that the p- methoxyphenyl-1, 2, 3-triazole moiety in 7b and 9b enhanced inhibitory activity against T. brucei, with 8b being more potent than nifurtimox, and having minimal toxicity towards mammalian cells.
benzimidazole ; 1, 2, 3-triazole ; resistant bacteria ; antiprotozoal activity ; Trypanosoma brucei ; MRSA
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Podaci o izdanju
33 (1)
2018.
1323-1334
objavljeno
1475-6366
1475-6374
10.1080/14756366.2018.1484733