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|Title:||Structure-activity relationships of antileishmanial and antimalarial chalcones||Authors:||Liu, M.
|Issue Date:||3-Jul-2003||Citation:||Liu, M., Wilairat, P., Croft, S.L., Tan, A.L.-C., Go, M.-L. (2003-07-03). Structure-activity relationships of antileishmanial and antimalarial chalcones. Bioorganic and Medicinal Chemistry 11 (13) : 2729-2738. ScholarBank@NUS Repository. https://doi.org/10.1016/S0968-0896(03)00233-5||Abstract:||A series of oxygenated chalcones which have been evaluated earlier for antimalarial activity (Plasmodium falciparum K1) were tested for antileishmanial activity against Leishmania donovani amastigotes. A comparison of structure-activity relationships reveal that different physicochemical and structural requirements exist for these two activities. Antileishmanial activity is associated with less lipophilic chalcones, in particular those with 4′-hydroxyl-substituted B rings and hetero/polyaromatic A rings. In contrast, chalcones with good antimalarial activity have alkoxylated B rings and electron-deficient A rings. Visualization of the steric and electrostatic fields generated from comparative molecular field analysis (CoMFA) indicate that the ring A of chalcones make a more significant contribution to antileishmanial activity while both rings A and B are important for antimalarial activity. Despite different requirements, two alkoxylated chalcones (8, 19) were identified which combined good antimalarial and antileishmanial activities. © 2003 Elsevier Science Ltd. All rights reserved.||Source Title:||Bioorganic and Medicinal Chemistry||URI:||http://scholarbank.nus.edu.sg/handle/10635/104865||ISSN:||09680896||DOI:||10.1016/S0968-0896(03)00233-5|
|Appears in Collections:||Staff Publications|
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