1. Academic Validation
  2. Oxazolo[3,2-a]pyridine. A new structural scaffold for the reversal of multi-drug resistance in Leishmania

Oxazolo[3,2-a]pyridine. A new structural scaffold for the reversal of multi-drug resistance in Leishmania

  • Bioorg Med Chem Lett. 2012 Oct 1;22(19):6272-5. doi: 10.1016/j.bmcl.2012.07.100.
Esther Caballero 1 José Ignacio Manzano Pilar Puebla Santiago Castanys Francisco Gamarro Arturo San Feliciano
Affiliations

Affiliation

  • 1 Departamento de Química Farmacéutica, Facultad de Farmacia, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain. escab@usal.es
Abstract

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.

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