Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
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 (Accepted Version)

Metadata
Show full item recordAbstract
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:
- Amer Chemical Soc, Washington
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:
- This is the peer-reviewed version of the following article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053
- The published version: http://cer.ihtm.bg.ac.rs/handle/123456789/2428
DOI: 10.1021/acsmedchemlett.8b00053
ISSN: 1948-5875
PubMed: 30034591