Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
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2018
Authors
Konstantinović, Jelena M.Videnović, Milica
Orsini, Stefania
Bogojević, Katarina
D'Alessandro, Sarah
Scaccabarozzi, Diletta
Terzić-Jovanović, Nataša
Gradoni, Luigi
Basilico, Nicoletta
Šolaja, Bogdan
Article (Published version)
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In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 LT 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 LT 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
Keywords:
Leishmania infantum / promastigote / amastigote / mice model / aminoquinolineSource:
Acs Medicinal Chemistry Letters, 2018, 9, 7, 629-634Publisher:
- American Chemical Society (ACS)
Funding / projects:
- The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-172008)
- Ministero dellIstruzione, dellUniversita e della Ricerca (PRIN) Project [20154JRJPP_004]
- Serbian Academy of Sciences and Arts, Executive Programme of Scientific and Technological Cooperation between the Italian Republic and the Republic of Serbia
Note:
- Peer-reviewed version: http://cer.ihtm.bg.ac.rs/handle/123456789/3626
DOI: 10.1021/acsmedchemlett.8b00053
ISSN: 1948-5875
PubMed: 30034591
WoS: 000442964000011
Scopus: 2-s2.0-85046787760
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IHTMTY - JOUR AU - Konstantinović, Jelena M. AU - Videnović, Milica AU - Orsini, Stefania AU - Bogojević, Katarina AU - D'Alessandro, Sarah AU - Scaccabarozzi, Diletta AU - Terzić-Jovanović, Nataša AU - Gradoni, Luigi AU - Basilico, Nicoletta AU - Šolaja, Bogdan PY - 2018 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/2428 AB - In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 LT 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 LT 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice. PB - American Chemical Society (ACS) T2 - Acs Medicinal Chemistry Letters T1 - Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice VL - 9 IS - 7 SP - 629 EP - 634 DO - 10.1021/acsmedchemlett.8b00053 ER -
@article{ author = "Konstantinović, Jelena M. and Videnović, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan", year = "2018", abstract = "In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50 LT 1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 LT 1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.", publisher = "American Chemical Society (ACS)", journal = "Acs Medicinal Chemistry Letters", title = "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice", volume = "9", number = "7", pages = "629-634", doi = "10.1021/acsmedchemlett.8b00053" }
Konstantinović, J. M., Videnović, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B.. (2018). Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in Acs Medicinal Chemistry Letters American Chemical Society (ACS)., 9(7), 629-634. https://doi.org/10.1021/acsmedchemlett.8b00053
Konstantinović JM, Videnović M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja B. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. in Acs Medicinal Chemistry Letters. 2018;9(7):629-634. doi:10.1021/acsmedchemlett.8b00053 .
Konstantinović, Jelena M., Videnović, Milica, Orsini, Stefania, Bogojević, Katarina, D'Alessandro, Sarah, Scaccabarozzi, Diletta, Terzić-Jovanović, Nataša, Gradoni, Luigi, Basilico, Nicoletta, Šolaja, Bogdan, "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice" in Acs Medicinal Chemistry Letters, 9, no. 7 (2018):629-634, https://doi.org/10.1021/acsmedchemlett.8b00053 . .