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Antileishmanial Effect of 1,5- and 1,8-Substituted Fused Naphthyridines.

Authors :
Melcón-Fernandez, Estela
Martín-Encinas, Endika
Palacios, Francisco
Galli, Gulio
Reguera, Rosa M.
Martínez-Valladares, María
Balaña-Fouce, Rafael
Alonso, Concepción
Pérez-Pertejo, Yolanda
Source :
Molecules; Jan2024, Vol. 29 Issue 1, p74, 16p
Publication Year :
2024

Abstract

In the absence of a vaccine, there is a need to find new drugs for the treatment of neglected tropical diseases, such as leishmaniasis, that can overcome the many drawbacks of those currently used. These disadvantages include cost, the need to maintain a cold chain, the route of administration, the associated adverse effects and the generation of resistance. In this work we have evaluated the antileishmanial effect of 1,5- and 1,8-substituted fused naphthyridines through in vitro and ex vivo assays, using genetically modified axenic and intramacrophagic Leishmania infantum amastigotes. The toxicity of these compounds has been tested in the mammalian host cell using murine splenic macrophages, as well as in murine intestinal organoids (miniguts) in order to assess their potential for oral administration. The 1,8- derivatives showed greater leishmanicidal activity and the presence of a nitrogen atom in the fused ring to the naphthyridine was important to increase the activity of both types of molecules. The aromatization of the pyridine ring also had marked differences in the activity of the compounds. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
14203049
Volume :
29
Issue :
1
Database :
Complementary Index
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
174716401
Full Text :
https://doi.org/10.3390/molecules29010074