In vitro leishmanicidal activity of lactone 1,4-dihydroquinoline derivatives against Leishmania (Leishmania) amazonensis

AbstractA series of lactone 1,4-dihydroquinoline derivatives4 (4 and4aa–4cm) was screened for in vitro antileishmanial activity against the promastigote form ofLeishmania (Leishmania) amazonensis. Screening results indicate that all of the synthesized compounds significantly reduced the growth of promastigote forms of promastigotes ofL. (L.) amazonensis. The cytotoxicity of the most active compounds was also measured on peritoneal macrophage cells. Compounds4ah and4bn showed better activities than other derivatives with IC50 values of 6.22 and 9.05  μM, respectively, with selectivity index 22 and 15 times less toxicity to macrophages cells than to parasites, respectively. The experimental data propose that the compounds may be further investigated against amastigote forms and may contribute to the search of new candidates drugs for treatmen t of cutaneous leishmaniasis.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research