Harmiquins, novel potent antiplasmodial hits (CROSBI ID 722889)
Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija
Podaci o odgovornosti
Rajić, Zrinka ; Poje, Goran ; Pessanha de Carvalho, Lais ; Held, Jana ; Perković, Ivana ; Tandarić, Tana ; Vianello, Robert
engleski
Harmiquins, novel potent antiplasmodial hits
Here we present design and synthesis of AT and TT harmiquins, evaluation of their biological activity and possible mechanism of action. Harmiquins displayed remarkable activity against the erythrocytic life stage of CQsensitive, as well as CQ-resistant Plasmodium strains. The most active compound, AT harmiquine 32, displayed a 5.5-fold higher activity against Pf3D7 than CQ (IC50 = 2 ± 0.3 nM), at least 15.9-fold higher activity than CQ against P. falciparum CQ resistant strains and had a very high selectivity index (4450). Two possible mechanisms of action, inhibition of heme polymerisation and binding to PfHsp90, might play a role in the inhibition of Plasmodium intraerythrocytic development.
harmine ; chloroquine ; hybrid molecules ; synthesis ; antiplasmodial activity ; PfHsp90
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Podaci o prilogu
224-225.
2022.
objavljeno
Podaci o matičnoj publikaciji
9th BBBB International Conference on Pharmaceutical Sciences, Book of Abstracts
Obreza, Aleš ; Dreu, Rok ; Zvonar Pobirk, Alenka ; Sterle Zorec, Barbara
Ljubljana: Slovensko farmacevtsko društvo in Univerza v Ljubljani, Fakulteta za farmacijo
Podaci o skupu
9th BBBB International Conference on Pharmaceutical Sciences Pharma: Sciences of Tomorrow
poster
15.09.2022-17.09.2022
Ljubljana, Slovenija