Videnović, Milica Đ.

Šolaja, Bogdan A.

Faculty of Chemistry Repository - Cherry

  &   52. savetovanje Srpskog hemijskog društva 134 OH P 20  Nova generacija 4-aminohinolina:  dizajn, sinteza i antimalarijska aktivnost Milica Đ. Videnović, Bogdan A. Šolaja* Inovacioni centar Hemijskog fakulteta u Beogradu, Beograd *Hemijski fakultet, Univerzitet u Beogradu, Studentski trg 12-16, Beograd  Malarija je infektivna bolest od koje je samo 2013. godine obolelo 198 miliona ljudi, sa smrtnim ishodom kod oko pola miliona pacijenata. Malariju izaziva parazit iz roda Plasmodium, koji na ljude prenosi ubodom ženka Anopheles komarca. Usled razvoja rezistencije parazita prema postojećim lekovima, postoji stalna potreba za pronalaženjem novih antimalarika. U nastavku naših istraživanja u oblasti dizajna i sinteze potencijalnih antimalarika sa različitim aromatičnim grupama kao nosačima aminohinolinske farmakofore,1a,b sintetisani su novi derivati 4-aminohinolina i ispitana njihova biološka aktivnost prema različitim sojevima P. falciparuma. Pokazana je zavisnost antimalarijske aktivnosti ispitanih jedinjenja od dužine alkil-niza i supstituenata na heterocikličnim jezgrima.  SNNNHNP. falciparum IC50 (nM)W2       D6      TM91C235   5           7             13  New generation of 4-aminoquinolines:  design, synthesis and antimalarial activity Milica Đ. Videnović, Bogdan A. Šolaja* Innovation center of the Faculty of Chemistry, Belgrade *Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, Belgrade  Malaria is an infectious disease resulting in 198 million estimated cases and over half a million deaths in 2013 alone. It is caused by the Plasmodium parasite transmitted among humans by female mosquitoes of the genus Anopheles. According to the development of parasite’s resistance to standard antimalarial drugs, there is a constant need for identification of new effective therapeutics. Following our previous results in the field of design and synthesis of potent antimalarials with an aromatic group as a carrier of aminoquinoline pharmacophore, we have synthesized new 4-aminoquinoline derivatives and discussed their in vitro antimalarial activities against three P. falciparum strains. We have shown that antimalarial activity depends on the length of alkyl linker and substitution pattern of heterocyclic cores.   Acknowledgment: This research was supported by the Ministry of Education, Science and Technological Development of Serbia (grant no. 172008)  1. a) Opsenica, I. M.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Šolaja, B. A.; J. Med. Chem. 2013, 56, 5860-5871; b) Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Đurković-Đaković, O.; Slavić, K.; Šolaja, B. A.; Bioorg. Med. Chem. 2015, 23, 2176-2186 

New generation of 4-aminoquinolines: design, synthesis and antimalarial activity

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New generation of 4-aminoquinolines: design, synthesis and antimalarial activity

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