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Título: | Oxazolo[3,2-a]pyridine. A new structural scaffold for the reversal of multi-drug resistance in Leishmania |
Autor: | Caballero, E.; Manzano, José Ignacio CSIC ORCID; Puebla, P.; Castanys, Santiago; Gamarro, Francisco; San Feliciano, A. | Fecha de publicación: | 2012 | Editor: | Pergamon Press | Citación: | Bioorganic and Medicinal Chemistry Letters 22: 6272- 6275 (2012) | Resumen: | Compounds belonging to three different classes of fused heterocyclic systems, structurally related to Calcium-channel blockers of the 1,4-dihydropyridine family, were evaluated in their ability to overcome leishmanial resistance to common drugs in a MDR Leishmania tropica strain. Compounds with the skeletal basis of oxazolo[3,2-a]pyridine displayed significant reversion of resistance to daunomycin and miltefosine, with reversion indexes up to 6.7-fold and 8.7-fold, respectively. Most interestingly, the enantiopure compound 20S attained to revert the resistance to both drugs and fairly more significantly than its enantiomer 20R. © 2012 Elsevier Ltd. All rights reserved. | URI: | http://hdl.handle.net/10261/80070 | DOI: | 10.1016/j.bmcl.2012.07.100 | Identificadores: | doi: 10.1016/j.bmcl.2012.07.100 issn: 0960-894X |
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