New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria
Novi derivati 4-aminohinolina kao umereni inhibitori parazita
2021
Аутори
Opsenica, IgorSelaković, Milica
Tot, Mikloš
Verbić, Tatjana
Srbljanović, Jelena
Štajner, Tijana
Đurković-Đaković, Olgica
Šolaja, Bogdan
Метаподаци
Приказ свих података о документуАпстракт
Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured.
Кључне речи:
quinoline / bromobenzyl derivatives / antimalarials / β-hematin inhibitory activityИзвор:
Journal of the Serbian Chemical Society, 2021, 86, 2, 115-123Издавач:
- Srpsko hemijsko društvo, Beograd
Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200168 (Универзитет у Београду, Хемијски факултет) (RS-MESTD-inst-2020-200168)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200288 (Иновациони центар Хемијског факултета у Београду доо) (RS-MESTD-inst-2020-200288)
- Serbian Academy of Sciences and Arts, project F-80
Институција/група
Institut za medicinska istraživanjaOpsenica, I., Selaković, M., Tot, M., Verbić, T., Srbljanović, J., Štajner, T., Đurković-Đaković, O.,& Šolaja, B.. (2021). New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society Srpsko hemijsko društvo, Beograd., 86(2), 115-123. https://doi.org/10.2298/JSC201225005O
Opsenica I, Selaković M, Tot M, Verbić T, Srbljanović J, Štajner T, Đurković-Đaković O, Šolaja B. New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society. 2021;86(2):115-123. doi:10.2298/JSC201225005O .
Opsenica, Igor, Selaković, Milica, Tot, Mikloš, Verbić, Tatjana, Srbljanović, Jelena, Štajner, Tijana, Đurković-Đaković, Olgica, Šolaja, Bogdan, "New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria" in Journal of the Serbian Chemical Society, 86, no. 2 (2021):115-123, https://doi.org/10.2298/JSC201225005O . .