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Pregled bibliografske jedinice broj: 998854

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


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, 2019. str. 145-145 (poster, domaća recenzija, sažetak, znanstveni)


CROSBI ID: 998854 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

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, 2019, 145-145

ISBN
9789536894673

Skup
26. Hrvatski skup kemičara i kemijskih inženjera

Mjesto i datum
Šibenik, Hrvatska, 9-12.04.2019

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



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2018-01-4682 - Novi spojevi temeljeni na bioizosterima purina za ispitivanje njihovih antitumorskih i antipatogenih djelovanja (PurBioCaPa) (Raić-Malić, Silvana, HRZZ)

Ustanove
Veterinarski fakultet, Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

Citiraj ovu publikaciju

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, 2019. str. 145-145 (poster, domaća recenzija, sažetak, znanstveni)
Bistrović, A., Stolić, I., Krstulović, L., Taylor, C., Kelly, M., Tomić, S., Bajić, M. & Raić-Malić, S. (2019) Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity. U: Galić, N. & Rogošić, M. (ur.)Knjiga sažetaka.
@article{article, year = {2019}, pages = {145-145}, keywords = {bis-benzimidazoles, ctDNA binding, UV-Vis, CD spectroscopy, thermal denaturation, Trypanosoma brucei}, isbn = {9789536894673}, title = {Novel symmetric bis-benzimidazoles: synthesis, DNA/RNA binding and antitrypanosomal activity}, keyword = {bis-benzimidazoles, ctDNA binding, UV-Vis, CD spectroscopy, thermal denaturation, Trypanosoma brucei}, publisher = {Hrvatsko dru\v{s}tvo kemijskih in\v{z}enjera i tehnologa}, publisherplace = {\v{S}ibenik, Hrvatska} }




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