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|Title:||Conformational and structural features determining in vitro antimalarial activity in some indolo[3,2-c]quinolines, anilinoquinolines and tetrahydroindolo[3,2-d]benzazepines||Authors:||Koh, H.
|Issue Date:||1994||Citation:||Koh, H.,Go, M.,Ngiam, T.,Mak, J. (1994). Conformational and structural features determining in vitro antimalarial activity in some indolo[3,2-c]quinolines, anilinoquinolines and tetrahydroindolo[3,2-d]benzazepines. European Journal of Medicinal Chemistry 29 (2) : 107-113. ScholarBank@NUS Repository.||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.||Source Title:||European Journal of Medicinal Chemistry||URI:||http://scholarbank.nus.edu.sg/handle/10635/105773||ISSN:||02235234|
|Appears in Collections:||Staff Publications|
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