TY  - JOUR
AU  - Rossier, Jeremie
AU  - Sovari, Sara Nasiri
AU  - Pavić, Aleksandar
AU  - Vojnović, Sandra
AU  - Stringer, Tameryn
AU  - Battig, Sarah
AU  - Smith, Gregory S.
AU  - Nikodinović-Runić, Jasmina
AU  - Zobi, Fabio
PY  - 2019
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1276
AB  - We have explored the possibility of using organometallic derivatives of cobalamin as a scaffold for the delivery of the same antimalarial drug to both erythro- and hepatocytes. This hybrid molecule approach, intended as a possible tool for the development of multi-stage antimalarial agents, pivots on the preparation of azide-functionalized drugs which, after coupling to the vitamin, are released with a 4-(4-ethynylphenyl)-triazole functionality. Three chloroquine and one imidazolopiperazine derivative (based on the KAF156 structure) were selected as model drugs. One hybrid chloroquine conjugate was extensively studied via fluorescent labelling for in vitro and in vivo bio-distribution studies and gave proof-of-concept for the design. It showed no toxicity in vivo (zebrafish model) as well as no hepatotoxicity, no cardiotoxicity or developmental toxicity of the embryos. All 4-(4-ethynylphenyl)-triazole derivatives of chloroquine were equally active against chloroquine-resistant (CQR) and chloroquine-sensitive (CQS) Plasmodium falciparum strains.
PB  - MDPI, Basel
T2  - Molecules
T1  - Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins
IS  - 12
VL  - 24
DO  - 10.3390/molecules24122310
ER  - 

@article{
author = "Rossier, Jeremie and Sovari, Sara Nasiri and Pavić, Aleksandar and Vojnović, Sandra and Stringer, Tameryn and Battig, Sarah and Smith, Gregory S. and Nikodinović-Runić, Jasmina and Zobi, Fabio",
year = "2019",
abstract = "We have explored the possibility of using organometallic derivatives of cobalamin as a scaffold for the delivery of the same antimalarial drug to both erythro- and hepatocytes. This hybrid molecule approach, intended as a possible tool for the development of multi-stage antimalarial agents, pivots on the preparation of azide-functionalized drugs which, after coupling to the vitamin, are released with a 4-(4-ethynylphenyl)-triazole functionality. Three chloroquine and one imidazolopiperazine derivative (based on the KAF156 structure) were selected as model drugs. One hybrid chloroquine conjugate was extensively studied via fluorescent labelling for in vitro and in vivo bio-distribution studies and gave proof-of-concept for the design. It showed no toxicity in vivo (zebrafish model) as well as no hepatotoxicity, no cardiotoxicity or developmental toxicity of the embryos. All 4-(4-ethynylphenyl)-triazole derivatives of chloroquine were equally active against chloroquine-resistant (CQR) and chloroquine-sensitive (CQS) Plasmodium falciparum strains.",
publisher = "MDPI, Basel",
journal = "Molecules",
title = "Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins",
number = "12",
volume = "24",
doi = "10.3390/molecules24122310"
}

Rossier, J., Sovari, S. N., Pavić, A., Vojnović, S., Stringer, T., Battig, S., Smith, G. S., Nikodinović-Runić, J.,& Zobi, F.. (2019). Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins. in Molecules
MDPI, Basel., 24(12).
https://doi.org/10.3390/molecules24122310

Rossier J, Sovari SN, Pavić A, Vojnović S, Stringer T, Battig S, Smith GS, Nikodinović-Runić J, Zobi F. Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins. in Molecules. 2019;24(12).
doi:10.3390/molecules24122310 .

Rossier, Jeremie, Sovari, Sara Nasiri, Pavić, Aleksandar, Vojnović, Sandra, Stringer, Tameryn, Battig, Sarah, Smith, Gregory S., Nikodinović-Runić, Jasmina, Zobi, Fabio, "Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins" in Molecules, 24, no. 12 (2019),
https://doi.org/10.3390/molecules24122310 . .