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|Title:||Structure-activity relationships of some indolo[3,2-c]quinolines with antimalarial activity|
|Authors:||Mei Lin Go|
Tong Lan Ngiam
Agnes Lay Choo Tan
National University of Singapore
|Keywords:||Pharmacology, Toxicology and Pharmaceutics|
|Citation:||European Journal of Pharmaceutical Sciences. Vol.6, No.1 (1998), 19-26|
|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.|
|Appears in Collections:||Scopus 1991-2000|
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