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Alternative Title
Abstract
A series of indolo[3,2-c]quinolines, anilinoquinolines and tetrahydroindolo[3,2-d]benzazepines, which differ in the conformational planarity of the key nuclei and the distance (N...N+) between the ring and side-chain nitrogen atoms, have been synthesized and evaluated in vitro against a number of isolates of Plasmodium falciparum. The results show that differences in conformational planarity of the indolo[3,2-c]quinoline (rigid), anilinoquinoline (flexible) and tetrahydroindolo[3,2-d]benzazepine (semi-rigid) nuclei have little effect on activity. However, the N...N+ distance is an important determinant of activity and analogues with a distance comparable to the N...N+ distance of amodiaquine and chloroquine demonstrated antimalarial activity. © 1994.
Keywords
anilinoquinoline, antimalarial activity, indolo[3,2-c]quinoline, SAR, tetrahydroindolo[3,2-d]benzazepine
Source Title
European Journal of Medicinal Chemistry
Publisher
Series/Report No.
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Date
1994
DOI
Type
Article