CER - Central Repository
Institute of Chemistry, Technology and Metallurgy
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrilic)
    • Serbian (Latin)
  • Login
View Item 
  •   Central Repository
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
  •   Central Repository
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice

Thumbnail
2018
ACC_2018_acsmedchemlett.8b00053.pdf (337.6Kb)
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 record
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.
Keywords:
Leishmania infantum / promastigote / amastigote / mice model / aminoquinoline
Source:
Acs Medicinal Chemistry Letters, 2018, 9, 7, 629-634
Publisher:
  • 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

WoS: 000442964000011

Scopus: 2-s2.0-85046787760
[ Google Scholar ]
6
5
URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3626
Collections
  • Radovi istraživača / Researchers' publications
Institution
IHTM

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

OpenAIRERCUB
 

 

All of DSpaceInstitutionsAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

OpenAIRERCUB