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Pregled bibliografske jedinice broj: 1016054

Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents


Beus, Maja; Fontinha, Diana; Held, Jana; Rajić, Zrinka; Uzelac, Lidija; Kralj, Marijeta; Prudêncio, Miguel; Zorc, Branka
Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents // Molecules, 24 (2019), 15; 2812, 15 doi:10.3390/molecules24152812 (međunarodna recenzija, članak, znanstveni)


Naslov
Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents

Autori
Beus, Maja ; Fontinha, Diana ; Held, Jana ; Rajić, Zrinka ; Uzelac, Lidija ; Kralj, Marijeta ; Prudêncio, Miguel ; Zorc, Branka

Izvornik
Molecules (1420-3049) 24 (2019), 15; 2812, 15

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Primaquine ; chloroquine ; antiplasmodial activity ; cytotoxicity ; fumardiamide

Sažetak
This paper describes a continuation of our efforts in the pursuit of novel antiplasmodial agents with optimized properties. Following our previous discovery of biologically potent asymmetric primaquine (PQ) and halogenaniline fumardiamides (1–6), we now report their significant in vitro activity against the hepatic stages of Plasmodium parasites. Furthermore, we successfully prepared chloroquine (CQ) analogue derivatives (11–16) and evaluated their activity against both the hepatic and erythrocytic stages of Plasmodium. Our results have shown that PQ fumardiamides (1–6) exert both higher activity against P. berghei hepatic stages and lower toxicity against human hepatoma cells than the parent drug and CQ derivatives (11–16). The favourable cytotoxicity profile of the most active compounds, 5 and 6, was corroborated by assays performed on human cells (human breast adenocarcinoma (MCF-7) and non-tumour embryonic kidney cells (HEK293T)), even when glucose-6- phosphate dehydrogenase (G6PD) was inhibited. The activity of CQ fumardiamides on P. falciparum erythrocytic stages was higher than that of PQ derivatives, comparable to CQ against CQ-resistant strain PfDd2, but lower than CQ when tested on the CQ-sensitive strain Pf3D7. In addition, both sets of compounds showed favourable drug-like properties. Hence, quinoline fumardiamides could serve as a starting point towards the development of safer and more effective antiplasmodial agents.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2013-5660
HRZZ-IP-2014-09-1501 - Dizajniranje, sinteza i evaluacija derivata primakina, vorinostata i sorafeniba kao potencijalnih citostatika
PTDC-SAU-INF-29550-2017

Ustanove
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb

Citiraj ovu publikaciju

Beus, Maja; Fontinha, Diana; Held, Jana; Rajić, Zrinka; Uzelac, Lidija; Kralj, Marijeta; Prudêncio, Miguel; Zorc, Branka
Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents // Molecules, 24 (2019), 15; 2812, 15 doi:10.3390/molecules24152812 (međunarodna recenzija, članak, znanstveni)
Beus, M., Fontinha, D., Held, J., Rajić, Z., Uzelac, L., Kralj, M., Prudêncio, M. & Zorc, B. (2019) Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents. Molecules, 24 (15), 2812, 15 doi:10.3390/molecules24152812.
@article{article, year = {2019}, pages = {15}, DOI = {10.3390/molecules24152812}, chapter = {2812}, keywords = {primaquine, chloroquine, antiplasmodial activity, cytotoxicity, fumardiamide}, journal = {Molecules}, doi = {10.3390/molecules24152812}, volume = {24}, number = {15}, issn = {1420-3049}, title = {Primaquine and Chloroquine Fumardiamides as Promising Antiplasmodial Agents}, keyword = {primaquine, chloroquine, antiplasmodial activity, cytotoxicity, fumardiamide}, chapternumber = {2812} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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