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Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides
Acta Pharmaceutica, 69 (2019), 2; 233-248. https://doi.org/10.2478/acph-2019-0019
Beus, Maja; Fonthina, Diana; Held, Jana; Rajić, Zrinka; Prudencio, Miguel; Zorc, Branka

Institucijski repozitorij: Repozitorij Farmaceutsko-biokemijskog fakulteta Sveučilišta u Zagrebu

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Beus, M., Fonthina, D., Held, J., Rajić, Z., Prudencio, M. i Zorc, B. (2019). Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides. Acta Pharmaceutica, 69. (2), 233-248. doi: 10.2478/acph-2019-0019

Beus, Maja, et al. "Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides." Acta Pharmaceutica, vol. 69, br. 2, 2019, str. 233-248. https://doi.org/10.2478/acph-2019-0019

Beus, Maja, Diana Fonthina, Jana Held, Zrinka Rajić, Miguel Prudencio i Branka Zorc. "Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides." Acta Pharmaceutica 69, br. 2 (2019): 233-248. https://doi.org/10.2478/acph-2019-0019

Beus, M., et al. (2019) 'Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides', Acta Pharmaceutica, 69(2), str. 233-248. doi: 10.2478/acph-2019-0019

Beus M, Fonthina D, Held J, Rajić Z, Prudencio M, Zorc B. Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides. Acta Pharmaceutica [Internet]. 2019. [pristupljeno 22.11.2024.];69(2):233-248. doi: 10.2478/acph-2019-0019

M. Beus, D. Fonthina, J. Held, Z. Rajić, M. Prudencio i B. Zorc, "Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides", Acta Pharmaceutica, vol. 69, br. 2, str. 233-248, 2019. [Online]. Dostupno na: https://urn.nsk.hr/urn:nbn:hr:163:062541. [Citirano: 22.11.2024.]

Za citiranje koristite ovu mrežnu adresu: https://urn.nsk.hr/urn:nbn:hr:163:062541
Podaci o radu
Naslov (engleski)Synthesis and antiplasmodial evaluation of novel mefloquine-based fumardiamides
AutorMaja Beus
AutorDiana Fonthina
AutorJana Held
AutorZrinka Rajić
AutorMiguel Prudencio
AutorBranka Zorc
Autorova ustanovaSveučilište u Zagrebu
Farmaceutsko-biokemijski fakultet
(Zavod za farmaceutsku kemiju)
Znanstveno / umjetničko
područje, polje i grana		BIOMEDICINA I ZDRAVSTVO
Farmacija
Farmacija
Sažetak (engleski)
The paper is focused on the synthesis and screening of the antiplasmodial activity of novel fumardiamides 5–10 with the mefloquine pharmacophore and a Michael acceptor motif. Multi-step reactions leading to the title compounds included two amide bond formations. The first amide bond was achieved by the reaction of (E)-ethyl 4-chloro-4-oxobut-2-enoate (1) and N1-(2,8-bis(trifluoromethyl)quinolin-4-yl)butane-1,4-diamine (2). The obtained ester 3 was hydrolysed and gave acid 4, which then reacted with the selected halogenanilines in the presence of HATU/DIEA and formed products 5–10. Title compounds showed marked, dose dependent activity in vitro against hepatic stages of Plasmodium berghei. IC50 values of the most active compounds 5, 7 and 9 bearing 3-fluoro, 3-chloro and 3-trifluoromethyl substituents were 3.04–4.16 µmol L–1, respectively. On the other hand, the compounds exerted only weak activity against the erythrocytic stages of two P. falciparum strains (Pf3D7 and PfDd2) in vitro, with the exception of compound 5 (IC50 = 2.9 µmol L–1).
Ključne riječi (engleski)
Jezikengleski
Vrsta publikacijeZnanstveni rad - Izvorni znanstveni rad
Status objaveObjavljen
Vrsta recenzijeRecenziran - međunarodna recenzija
Verzija publikacijeObjavljena verzija rada (izdavačev PDF)
Naslov časopisaActa Pharmaceutica
Brojčani podacivol. 69, br. 2, str. 233-248
p-ISSN1330-0075
e-ISSN1846-9558
DOIhttps://doi.org/10.2478/acph-2019-0019
URN:NBNurn:nbn:hr:163:062541
Datum objave publikacije2019
URL dokumentahttps://hrcak.srce.hr/217028
Vrsta resursaTekst
Prava pristupaOtvoreni pristup
Uvjeti korištenjaIkona licence Zaštićeno autorskim pravom.
Datum i vrijeme pohrane2019-03-08 16:22:52