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Title: Structure-activity relationships of some indolo[3,2-c]quinolines with antimalarial activity
Authors: Go, M.-L. 
Ngiam, T.-L. 
Tan, A.L.-C. 
Kuaha, K.
Wilairat, P.
Keywords: Antimalarial activity
Structure-activity relationships
Issue Date: Jan-1998
Citation: Go, M.-L., Ngiam, T.-L., Tan, A.L.-C., Kuaha, K., Wilairat, P. (1998-01). Structure-activity relationships of some indolo[3,2-c]quinolines with antimalarial activity. European Journal of Pharmaceutical Sciences 6 (1) : 19-26. ScholarBank@NUS Repository.
Abstract: The synthesis, physicochemical characterization and in vitro antimalarial activity of a series of indolo[3,2-c]quinolines (9a-f) are described. There is only a poor correlation between the activity and hydrophobicity. In contrast, 33% of the observed variation in antimalarial activity can be attributed to the size of the side chain attached to position 9 of the indoloquinoline ring. An increase in the size of this dibasic side chain generally results in a reduction in activity, suggesting that it is accommodated in a site/cavity of limited size on the receptor. More significantly, the charge on the distal nitrogen (N3) on the side chain, located 10-11 Å from the quinoline N, could account for 75% of the observed variation. Since a large charge on N3 is associated with improved antimalarial activity, it is suggested that N3 is protonated and functions as a H bond donor in the drug-receptor interaction.
Source Title: European Journal of Pharmaceutical Sciences
ISSN: 09280987
DOI: 10.1016/S0928-0987(97)00064-X
Appears in Collections:Staff Publications

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