Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
Samo za registrovane korisnike
2018
Autori
Konstantinović, Jelena M.Videnović, Milica
Orsini, Stefania
Bogojević, Katarina
D'Alessandro, Sarah
Scaccabarozzi, Diletta
Terzić-Jovanović, Nataša
Gradoni, Luigi
Basilico, Nicoletta
Šolaja, Bogdan
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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.
Ključne reči:
Leishmania infantum / promastigote / amastigote / mice model / aminoquinolineIzvor:
Acs Medicinal Chemistry Letters, 2018, 9, 7, 629-634Izdavač:
- American Chemical Society (ACS)
Finansiranje / projekti:
- Sinteza aminohinolina i njihovih derivata kao antimalarika i inhibitora botulinum neurotoksina A (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
Napomena:
- 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
Institucija/grupa
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 . .