Naslov
Antiplasmodial activity of triazole-type harmiquins

Autori
Poje, Goran ; Perković, Ivana ; Held, Jana ; Rajić, Zrinka

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
27th Croatian Meeting of Chemists and Chemical Engineers, Book of Abstracts / Marković, Dean ; Meštrović, Ernest ; Namjesnik, Danijel ; Tomašić, Vesna - Zagreb : Hrvatsko kemijsko društvo, 2021, 167-167

Skup
27. hrvatski skup kemičara i kemijskih inženjera (27HSKIKI)

Mjesto i datum
Veli Lošinj, Hrvatska, 05.10.2021. - 08.10.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
malaria, hybrid molecules, harmine, chloroquine

Sažetak
Global malaria control is being disrupted by the emergence of drug resistance to most of the available antimalarials, necessitating the search for novel drugs.[1] A recent rational approach used in the antimalarial drug design involves linking two bioactive molecules into a single chemical entity, i. e. preparing hybrid compounds.[2] Herein, we represent harmiquins, hybrids constituted of two moieties with pronounced antimalarial properties, -carboline alkaloid harmine and 7-chloroquinoline, [2, 3] linked via 1H-1, 2, 3-triazole (Figure). Antimalarial activity of novel hybrids was evaluated in vitro against the erythrocytic stage of the Plasmodium life cycle, revealing compound 8 as the most active (IC50 value 11.6±3.8 nM). Furthermore, the diversity of harmiquins allowed us to draw several conclusions about the structure-activity relationship: 1) the activity decreased following the pattern of the -carboline core substitution N-9 > O-7 > O6 > C-3 > C-1, 2) hybrids containing aminoethylene linker (compounds 6-8) exerted more pronounced antimalarial activity.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija

POVEZANOST RADA