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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

Bistrović, Andrea ; Stolić, Ivana ; Krstulović, Luka ; Taylor, C. Martin ; Kelly, M. John ; Tomić, Sanja ; Bajić, Miroslav ; Raić-Malić, Silvana Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity // Knjiga sažetaka / Galić, Nives ; Rogošić, Marko (ur.). Zagreb: Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2019. str. 145-145

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

Povezanost rada

Kemija