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Title: Structure-activity relationships of antileishmanial and antimalarial chalcones
Authors: Liu, M.
Wilairat, P.
Croft, S.L.
Tan, A.L.-C. 
Go, M.-L. 
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.
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
ISSN: 09680896
DOI: 10.1016/S0968-0896(03)00233-5
Appears in Collections:Staff Publications

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