prikaz prve stranice dokumenta A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides
  Preuzmi
PDF 7.84 MB
Znanstveni rad - Izvorni znanstveni rad
A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides
British Journal of Pharmacology, 178 (2021), 2; 363-377. https://doi.org/10.1111/bph.15292
Perić, Mihaela; Pešić, Dijana; Alihodžić, Sulejman; Fajdetić, Andrea; Herreros, Esperanza; Gamo, Francisco Javier; Angulo‐Barturen, Iñigo; Jiménez‐Díaz, María Belén; Ferrer‐Bazaga, Santiago; Martínez, María S.; Gargallo‐Viola, Domingo; Mathis, Amanda; Kessler, Albane; Banjanac, Mihailo; Padovan, Jasna; Bencetić Mihaljević, Vlatka; Munić Kos, Vesna; Bukvić, Mirjana; Eraković Haber, Vesna; Spaventi, Radan Više autora...

Citirajte ovaj rad

Perić, M., Pešić, D., Alihodžić, S., Fajdetić, A., Herreros, E., Gamo, F. J. ... Spaventi, R. (2021). A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides. British Journal of Pharmacology, 178. (2), 363-377. doi: 10.1111/bph.15292

Perić, Mihaela, et al. "A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides." British Journal of Pharmacology, vol. 178, br. 2, 2021, str. 363-377. https://doi.org/10.1111/bph.15292

Perić, Mihaela, Dijana Pešić, Sulejman Alihodžić, Andrea Fajdetić, Esperanza Herreros, Francisco Javier Gamo, Iñigo Angulo‐Barturen, et al. "A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides." British Journal of Pharmacology 178, br. 2 (2021): 363-377. https://doi.org/10.1111/bph.15292

Perić, M., et al. (2021) 'A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides', British Journal of Pharmacology, 178(2), str. 363-377. doi: 10.1111/bph.15292

Perić M, Pešić D, Alihodžić S, Fajdetić A, Herreros E, Gamo FJ, i sur.. A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides. British Journal of Pharmacology [Internet]. 01.2021. [pristupljeno 05.05.2024.];178(2):363-377. doi: 10.1111/bph.15292

M. Perić, et al., "A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides", British Journal of Pharmacology, vol. 178, br. 2, str. 363-377, Siječanj 2021. [Online]. Dostupno na: https://urn.nsk.hr/urn:nbn:hr:105:763145. [Citirano: 05.05.2024.]

Za citiranje koristite ovu mrežnu adresu: https://urn.nsk.hr/urn:nbn:hr:105:763145
Prijavite se u repozitorij kako biste mogli spremiti objekt u svoju listu.
Podaci o radu
Naslov (engleski)A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides
AutorMihaela Perić
MBZ: 222361
AutorDijana Pešić
AutorSulejman Alihodžić
AutorAndrea Fajdetić
AutorEsperanza Herreros
AutorFrancisco Javier Gamo
AutorIñigo Angulo‐Barturen
AutorMaría Belén Jiménez‐Díaz
AutorSantiago Ferrer‐Bazaga
AutorMaría S. Martínez
AutorDomingo Gargallo‐Viola
AutorAmanda Mathis
AutorAlbane Kessler
AutorMihailo Banjanac
AutorJasna Padovan
AutorVlatka Bencetić Mihaljević
AutorVesna Munić Kos
AutorMirjana Bukvić
AutorVesna Eraković Haber
AutorRadan Spaventi
Autorova ustanovaSveučilište u Zagrebu
Medicinski fakultet
Znanstveno / umjetničko
područje, polje i grana		BIOMEDICINA I ZDRAVSTVO
Temeljne medicinske znanosti
Sažetak (engleski)
Background and purpose: Efficacy of current antimalarial treatments is declining as a result of increasing antimalarial drug resistance, so new and potent antimalarial drugs are urgently needed. Azithromycin, an azalide antibiotic, was found useful in malaria therapy, but its efficacy in humans is low. ----- Experimental approach: Four compounds belonging to structurally different azalide classes were tested and their activities compared to azithromycin and chloroquine. in vitro evaluation included testing against sensitive and resistant Plasmodium falciparum, cytotoxicity against HepG2 cells, accumulation and retention in human erythrocytes, antibacterial activity, and mode of action studies (delayed death phenotype and haem polymerization). in vivo assessment enabled determination of pharmacokinetic profiles in mice, rats, dogs, and monkeys and in vivo efficacy in a humanized mouse model. ----- Key results: Novel fast-acting azalides were highly active in vitro against P. falciparum strains exhibiting various resistance patterns, including chloroquine-resistant strains. Excellent antimalarial activity was confirmed in a P. falciparum murine model by strong inhibition of haemozoin-containing trophozoites and quick clearance of parasites from the blood. Pharmacokinetic analysis revealed that compounds are metabolically stable and have moderate oral bioavailability, long half-lives, low clearance, and substantial exposures, with blood cells as the preferred compartment, especially infected erythrocytes. Fast anti-plasmodial action is achieved by the high accumulation into infected erythrocytes and interference with parasite haem polymerization, a mode of action different from slow-acting azithromycin. ----- Conclusion and implications: The hybrid derivatives described here represent excellent antimalarial drug candidates with the potential for clinical use in malaria therapy.
Ključne riječi (engleski)
Jezikengleski
Vrsta publikacijeZnanstveni rad - Izvorni znanstveni rad
Status objaveObjavljen
Vrsta recenzijeRecenziran
Verzija publikacijeObjavljena verzija rada (izdavačev PDF)
Naslov časopisaBritish Journal of Pharmacology
Brojčani podacivol. 178, br. 2, str. 363-377
p-ISSN0007-1188
e-ISSN1476-5381
DOIhttps://doi.org/10.1111/bph.15292
URN:NBNurn:nbn:hr:105:763145
Datum objave publikacije2021-01
URL dokumentahttps://onlinelibrary.wiley.com/doi/10.1111/bph.15292
Vrsta resursaTekst
Prava pristupaOtvoreni pristup
Uvjeti korištenjaIkona licence Imenovanje 4.0 međunarodna (CC BY 4.0)
Datum i vrijeme pohrane2022-02-07 08:21:41