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 < 1 μM against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 < 1 μM 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.
Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice / J. Konstantinović, M. Videnović, S. Orsini, K. Bogojević, S. D'Alessandro, D. Scaccabarozzi, N. Terzić Jovanović, L. Gradoni, N. Basilico, B.A. Šolaja. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 9:7(2018 Jul 12), pp. 629-634.
Titolo: | Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice |
Autori: | |
Parole Chiave: | Leishmania infantum; promastigote; amastigote; mice model; aminoquinoline |
Settore Scientifico Disciplinare: | Settore MED/04 - Patologia Generale Settore MED/07 - Microbiologia e Microbiologia Clinica |
Progetto: | Towards multi-stage drugs to fight poverty related and neglected parasitic diseases: synthetic and natural compounds directed against Leishmania, Plasmodium and Schistosoma life stages and assessment of their mechanisms of action. |
Data di pubblicazione: | 12-lug-2018 |
Rivista: | |
Tipologia: | Article (author) |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/acsmedchemlett.8b00053 |
Appare nelle tipologie: | 01 - Articolo su periodico |
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