Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity (CROSBI ID 675738)
Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | domaća recenzija
Podaci o odgovornosti
Bistrović, Andrea ; Stolić, Ivana ; Krstulović, Luka ; Taylor, C. Martin ; Kelly, M. John ; Tomić, Sanja ; Bajić, Miroslav ; Raić-Malić, Silvana
engleski
Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity
Human African trypanosomiasis (HAT), or sleeping sickness, is one of the most deadly neglected tropical diseases (NTDs), with 65 million people at risk in 36 countries [1]. Current therapies for HAT are unsatisfactory and under threat from emerging resistance [2]. In continuation of our recent work on the development of aromatic amidines as DNA-binding ligands and anti- trypanosomal agents [3], we aimed here to expand the benzimidazole scaffold to 5-membered furyl and 1, 2, 3-triazolyl moieties that may adopt helical topology to approximately match the curvature of DNA in the minor groove. The novel benzimidazol-2-yl-fur- 5-yl-(1, 2, 3)- triazolyl dimeric series with aliphatic and aromatic central linkers was successfully prepared with the aim of assessing binding affinity to DNA/RNA and antitrypanosomal activity. The bis- benzimidazole imidazoline 15c, with antitrypanosomal potency in the submicromolar range and DNA interacting properties, emerged as a candidate for further structural optimization to obtain more effective agents to combat trypanosome infections.
bis-benzimidazoles ; ctDNA binding ; UV-Vis ; CD spectroscopy ; thermal denaturation ; Trypanosoma brucei
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Podaci o prilogu
145-145.
2019.
objavljeno
Podaci o matičnoj publikaciji
Knjiga sažetaka
Galić, Nives ; Rogošić, Marko
Zagreb: Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI)
9789536894673
Podaci o skupu
26. hrvatski skup kemičara i kemijskih inženjera (26HSKIKI) ; 4. simpozij Vladimir Prelog
poster
09.04.2019-12.04.2019
Šibenik, Hrvatska