O -geranylchalcones: synthesis and metabolic inhibition against Leishmania mexicana and Trypanosoma cruzi

AbstractIn this paper, twelve substitutedO-geranylchalcones were synthesized and evaluated for their leishmanicidal and trypanocidal activity. All the synthesized compounds showed selective activity againstL. mexicana strain in comparison toT. cruzi strain.O-geranyl chalcone5j substituted with ameta-NO2 group in B ring, showed the highest selectivity (IS  = 21.46). Cytotoxicity studies using murine macrophages J774.A1 showed that F and Cl substituents on thepara position on the B ring, displayed the less toxicity as in compounds5f and5i. Calculated ADME properties indicated that the obtained chalcones presented a good skin permeability, making them adequate candidates for local treatment of cutaneous leishmaniasis.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research