Naslov
Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity

Autori
Bistrović, Andrea ; Stolić, Ivana ; Krstulović, Luka ; Taylor, C. Martin ; Kelly, M. John ; Tomić, Sanja ; Bajić, Miroslav ; Raić-Malić, Silvana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Knjiga sažetaka / Galić, Nives ; Rogošić, Marko - Zagreb : Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2019, 145-145

ISBN
9789536894673

Skup
26. hrvatski skup kemičara i kemijskih inženjera (26HSKIKI) ; 4. simpozij Vladimir Prelog

Mjesto i datum
Šibenik, Hrvatska, 09.04.2019. - 12.04.2019

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
bis-benzimidazoles ; ctDNA binding ; UV-Vis ; CD spectroscopy ; thermal denaturation ; Trypanosoma brucei

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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