NATO [SfP983638]

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NATO [SfP983638]

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Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077

Opsenica, Igor; Tot, Mikloš; Gomba, Laura; Nuss, Jonathan E.; Sciotti, Richard J.; Bavari, Sina; Burnett, James C.; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2013)

TY  - DATA
AU  - Opsenica, Igor
AU  - Tot, Mikloš
AU  - Gomba, Laura
AU  - Nuss, Jonathan E.
AU  - Sciotti, Richard J.
AU  - Bavari, Sina
AU  - Burnett, James C.
AU  - Šolaja, Bogdan A.
PY  - 2013
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3465
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3465
ER  - 
@misc{
author = "Opsenica, Igor and Tot, Mikloš and Gomba, Laura and Nuss, Jonathan E. and Sciotti, Richard J. and Bavari, Sina and Burnett, James C. and Šolaja, Bogdan A.",
year = "2013",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3465"
}
Opsenica, I., Tot, M., Gomba, L., Nuss, J. E., Sciotti, R. J., Bavari, S., Burnett, J. C.,& Šolaja, B. A.. (2013). Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077. in Journal of Medicinal Chemistry
Amer Chemical Soc, Washington..
https://hdl.handle.net/21.15107/rcub_cherry_3465
Opsenica I, Tot M, Gomba L, Nuss JE, Sciotti RJ, Bavari S, Burnett JC, Šolaja BA. Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077. in Journal of Medicinal Chemistry. 2013;.
https://hdl.handle.net/21.15107/rcub_cherry_3465 .
Opsenica, Igor, Tot, Mikloš, Gomba, Laura, Nuss, Jonathan E., Sciotti, Richard J., Bavari, Sina, Burnett, James C., Šolaja, Bogdan A., "Supplementary data for article: Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J. E.; Sciotti, R. J.; Bavari, S.; Burnett, J. C.; Šolaja, B. A. 4-Amino-7-Chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. Journal of Medicinal Chemistry 2013, 56 (14), 5860–5871. https://doi.org/10.1021/jm4006077" in Journal of Medicinal Chemistry (2013),
https://hdl.handle.net/21.15107/rcub_cherry_3465 .

4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity

Opsenica, Igor; Tot, Mikloš; Gomba, Laura; Nuss, Jonathan E.; Sciotti, Richard J.; Bavari, Sina; Burnett, James C.; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2013)

TY  - JOUR
AU  - Opsenica, Igor
AU  - Tot, Mikloš
AU  - Gomba, Laura
AU  - Nuss, Jonathan E.
AU  - Sciotti, Richard J.
AU  - Bavari, Sina
AU  - Burnett, James C.
AU  - Šolaja, Bogdan A.
PY  - 2013
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/1381
AB  - Structurally simplified analogues of dual antimalarial and botulinum neurotoxin serotype A light chain (BoNT/A LC) inhibitor bis-aminoquinoline (1) were prepared. New compounds were designed to improve ligand efficiency while maintaining or exceeding the inhibitory potency of 1. Three of the new compounds are more active than 1 against both indications. Metabolically, the new inhibitors are relatively stable and nontoxic. 12, 14, and 15 are more potent BoNT/A LC inhibitors than 1. Additionally, 15 has excellent in vitro antimalarial efficacy, with IC90 values ranging from 4.45 to 12.11 nM against five Plasmodium falciparum (Pf) strains: W2, D6, C235, C2A, and C2B. The results indicate that the same level of inhibitory efficacy provided by 1 can be retained/exceeded with less structural complexity. 12, 14, and 15 provide new platforms for the development of more potent dual BoNT/A LC and P.f. inhibitors adhering to generally accepted chemical properties associated with the druggability of synthetic molecules.
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - 4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity
VL  - 56
IS  - 14
SP  - 5860
EP  - 5871
DO  - 10.1021/jm4006077
ER  - 
@article{
author = "Opsenica, Igor and Tot, Mikloš and Gomba, Laura and Nuss, Jonathan E. and Sciotti, Richard J. and Bavari, Sina and Burnett, James C. and Šolaja, Bogdan A.",
year = "2013",
abstract = "Structurally simplified analogues of dual antimalarial and botulinum neurotoxin serotype A light chain (BoNT/A LC) inhibitor bis-aminoquinoline (1) were prepared. New compounds were designed to improve ligand efficiency while maintaining or exceeding the inhibitory potency of 1. Three of the new compounds are more active than 1 against both indications. Metabolically, the new inhibitors are relatively stable and nontoxic. 12, 14, and 15 are more potent BoNT/A LC inhibitors than 1. Additionally, 15 has excellent in vitro antimalarial efficacy, with IC90 values ranging from 4.45 to 12.11 nM against five Plasmodium falciparum (Pf) strains: W2, D6, C235, C2A, and C2B. The results indicate that the same level of inhibitory efficacy provided by 1 can be retained/exceeded with less structural complexity. 12, 14, and 15 provide new platforms for the development of more potent dual BoNT/A LC and P.f. inhibitors adhering to generally accepted chemical properties associated with the druggability of synthetic molecules.",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity",
volume = "56",
number = "14",
pages = "5860-5871",
doi = "10.1021/jm4006077"
}
Opsenica, I., Tot, M., Gomba, L., Nuss, J. E., Sciotti, R. J., Bavari, S., Burnett, J. C.,& Šolaja, B. A.. (2013). 4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. in Journal of Medicinal Chemistry
Amer Chemical Soc, Washington., 56(14), 5860-5871.
https://doi.org/10.1021/jm4006077
Opsenica I, Tot M, Gomba L, Nuss JE, Sciotti RJ, Bavari S, Burnett JC, Šolaja BA. 4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity. in Journal of Medicinal Chemistry. 2013;56(14):5860-5871.
doi:10.1021/jm4006077 .
Opsenica, Igor, Tot, Mikloš, Gomba, Laura, Nuss, Jonathan E., Sciotti, Richard J., Bavari, Sina, Burnett, James C., Šolaja, Bogdan A., "4-Amino-7-chloroquinolines: Probing Ligand Efficiency Provides Botulinum Neurotoxin Serotype A Light Chain Inhibitors with Significant Antiprotozoal Activity" in Journal of Medicinal Chemistry, 56, no. 14 (2013):5860-5871,
https://doi.org/10.1021/jm4006077 . .
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