A wide variety of biologically active compounds contain indole and quinoline nuclei. A one step synthesis of some novel indolyl quinoline analogs e.g. 2-(2'-Dichloro-acetamidobenzyl)-3-(3' -indolyl)quinoline , 2-(2'-Dichloroacetamido-5'-bromo- benzyl)-3'-[3'-(5'-bromoindolyl)]-6-bromo quinoline , and 2-(2'-acetamido benzyl)-3-(3'-indolyl)-quinoline  has been developed under Friedel-Crafts acylation conditions. The compounds inhibit the relaxation and decatenation reactions catalysed by type I and type II DNA topoisomerases of Leishmania donovani. Among the three synthetic indolyl quinolines, the Br-derivative  is most active. The results reported here concerning the inhibition of type I and type II DNA topoisomerases indicate that the compounds act as 'dual inhibitors' of the enzymes and can be exploited for rational drug design in human leishmaniasis.
|Original language||English (US)|
|Number of pages||5|
|Journal||Biochemical and Biophysical Research Communications|
|State||Published - Jan 3 1997|
ASJC Scopus subject areas
- Molecular Biology
- Cell Biology