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

Abstract

A series of lactone 1,4-dihydroquinoline derivatives 4 (4 and 4aa-4cm) was screened for in vitro antileishmanial activity against the promastigote form of Leishmania (Leishmania) amazonensis. Screening results indicate that all of the synthesized compounds significantly reduced the growth of promastigote forms of promastigotes of L. (L.) amazonensis. The cytotoxicity of the most active compounds was also measured on peritoneal macrophage cells. Compounds 4ah and 4bn showed better activities than other derivatives with IC 50 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 treatment of cutaneous leishmaniasis.

Kinetic Resolution of 2‐Aryldihydroquinolines Using Lithiation – Synthesis of Chiral 1,2‐ and 1,4‐Dihydroquinolines

“…[2] In contrast, the related dihydroquinoline ring system has received relatively little attention. This is despite their potential as drugs or prodrugs,[ 3 , 4 , 5 , 6 ] and their usefulness as intermediates towards the synthesis of quinolines or tetrahydroquinolines.…”