New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria
Novi derivati 4-aminohinolina kao umereni inhibitori parazita
MetadataShow full item record
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.
Keywords:quinoline / bromobenzyl derivatives / antimalarials / β-hematin inhibitory activity
Source:Journal of the Serbian Chemical Society, 2021, 86, 2, 115-123
- Srpsko hemijsko društvo, Beograd
Funding / projects:
- Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 200168 (University of Belgrade, Faculty of Chemistry) (RS-200168)
- Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 200288 (Innovation Center of the Faculty of Chemistry) (RS-200288)
- Serbian Academy of Sciences and Arts, project F-80
WoS: 000639574500001[ Google Scholar ]
Institution/CommunityInstitut za medicinska istraživanja
Opsenica, 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 conv_5520
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 conv_5520 .
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 ., conv_5520 .