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Pregled bibliografske jedinice broj: 572659

Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents


Starčević, Kristina; Pešić, Dijana; Toplak, Ana; Landek, Goran; Alihodžić, Sulejman; Herreros, Esperanza; Ferrer, Santiago; Spaventi, Radan; Perić, Mihaela
Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents // European journal of medicinal chemistry, 49 (2012), 365-378 doi:10.1016/j.ejmech.2012.01.039 (međunarodna recenzija, članak, znanstveni)


Naslov
Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents

Autori
Starčević, Kristina ; Pešić, Dijana ; Toplak, Ana ; Landek, Goran ; Alihodžić, Sulejman ; Herreros, Esperanza ; Ferrer, Santiago ; Spaventi, Radan ; Perić, Mihaela

Izvornik
European journal of medicinal chemistry (0223-5234) 49 (2012); 365-378

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

Ključne riječi
malaria; antimalarial; azalide; quinoline; hybrid molecules; synthesis; Plasmodium falciparum

Sažetak
Malaria remains the most prevalent tropical disease, and due to the spread of resistant parasites novel therapeutics are urgently needed. Azithromycin has shown potential in malaria treatment so we designed hybrid azalide molecules with the aim to improve activity against and selectivity for the malaria parasite. Novel hybrid molecules comprising 4-aminoquinoline moiety covalently liked to 15-membered azalide scaffold at position C-30 were synthesized and biologically evaluated. Antimalarial testing against Plasmodium falciparum sensitive and resistant strains confirmed the improved in vitro activity over azithromycin and chloroquine. Selectivity of the compounds (HepG2 IC50/P. falciparum IC50 ratio) for the parasitewas high (100e2700) and their antibacterial activity diminished. Even though oral bioavailability determined for compound 12 was low, novel quinoline C-30-substituted 15-membered azalides represent an interesting subclass of antimalarial macrolides that need further research and evaluation.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
053-0531854-1849 - Udio tkiva, kemijski i masnokiselinski sastav mesa simentalske pasmine goveda (Igor Štoković, )
053-0982914-2965 - Dizajn i sinteza bisamidina sa protutumorskim djelovanjem (Miroslav Bajić, )

Ustanove
Veterinarski fakultet, Zagreb,
Medicinski fakultet, Zagreb,
Fidelta d.o.o.

Citiraj ovu publikaciju

Starčević, Kristina; Pešić, Dijana; Toplak, Ana; Landek, Goran; Alihodžić, Sulejman; Herreros, Esperanza; Ferrer, Santiago; Spaventi, Radan; Perić, Mihaela
Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents // European journal of medicinal chemistry, 49 (2012), 365-378 doi:10.1016/j.ejmech.2012.01.039 (međunarodna recenzija, članak, znanstveni)
Starčević, K., Pešić, D., Toplak, A., Landek, G., Alihodžić, S., Herreros, E., Ferrer, S., Spaventi, R. & Perić, M. (2012) Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents. European journal of medicinal chemistry, 49, 365-378 doi:10.1016/j.ejmech.2012.01.039.
@article{article, year = {2012}, pages = {365-378}, DOI = {10.1016/j.ejmech.2012.01.039}, keywords = {malaria, antimalarial, azalide, quinoline, hybrid molecules, synthesis, Plasmodium falciparum}, journal = {European journal of medicinal chemistry}, doi = {10.1016/j.ejmech.2012.01.039}, volume = {49}, issn = {0223-5234}, title = {Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents}, keyword = {malaria, antimalarial, azalide, quinoline, hybrid molecules, synthesis, Plasmodium falciparum} }

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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