Leishmanicidal activity of aliphatic and aromatic lactones: correlation structure-activity.
Several aliphatic and aromatic lactones and two dimers were synthesized using the sequence: allylation - esterification - metathesis. These compounds were active in vitro against intracellular amastigotes of Leishmania panamensis. The structure-activity relationship showed the importance of the aliphatic side chain to enhance the biological activity and to obtain lower cytotoxicity. It was also observed that a decrease in the size of the lactone ring increases the selectivity index.
Castaño
Marcela
M
Grupo de Química Orgánica de Productos Naturales-SIU, Universidad de Antioquia, P.O. Box 1226, Medellín, Colombia.
Cardona
Wilson
W
Quiñones
Winston
W
Robledo
Sara
S
Echeverri
Fernando
F
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018334:Leishmania guyanensis / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D007783:Lactones