M. Go, H. Koh, T. Ngiam
Jun 1, 1992
Citations
0
Influential Citations
14
Citations
Quality indicators
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract A series of indolo[3,2-c]quinolines (1b–e) was synthesized by Fischer indolization of 7-chloro-1,2,3,4-tetrahydroquinolin-4-one with the appropriate hydrazines (7b–e). Evaluation of in vitro antimalarial activity was carried out against a chloroquine resistant strain of Plasmodium falciparum. Except for compound 1e which lacked a basic side chain at position 9, the other indolo[3,2-c]quinolines 1b–d were active. The most active compound was 3-chloro-8-methoxy-9-(4-methyl-1-piperazinylmethyl)-11H-indolo[3,2-c]quinoline (1d) trihydrochloride which was about 104 times more active than chloroquine in vitro. The effects of structural variation on antimalarial activity were discussed.