Please use this identifier to cite or link to this item: https://doi.org/10.1016/S0928-0987(97)00064-X
DC FieldValue
dc.titleStructure-activity relationships of some indolo[3,2-c]quinolines with antimalarial activity
dc.contributor.authorGo, M.-L.
dc.contributor.authorNgiam, T.-L.
dc.contributor.authorTan, A.L.-C.
dc.contributor.authorKuaha, K.
dc.contributor.authorWilairat, P.
dc.date.accessioned2014-10-28T03:12:49Z
dc.date.available2014-10-28T03:12:49Z
dc.date.issued1998-01
dc.identifier.citationGo, 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. https://doi.org/10.1016/S0928-0987(97)00064-X
dc.identifier.issn09280987
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/104866
dc.description.abstractThe 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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/S0928-0987(97)00064-X
dc.sourceScopus
dc.subjectAntimalarial activity
dc.subjectIndoloquinolines
dc.subjectStructure-activity relationships
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.contributor.departmentCOMPUTATIONAL SCIENCE
dc.description.doi10.1016/S0928-0987(97)00064-X
dc.description.sourcetitleEuropean Journal of Pharmaceutical Sciences
dc.description.volume6
dc.description.issue1
dc.description.page19-26
dc.description.codenEPSCE
dc.identifier.isiut000071877100003
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