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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.
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
January 2013,
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Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
October 2001,
Archiv der Pharmazie,
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
September 2002,
Bioorganic & medicinal chemistry letters,
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
March 2007,
Medicinal chemistry (Shariqah (United Arab Emirates)),
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
November 1998,
Journal of medicinal chemistry,
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
February 2010,
Bioorganic & medicinal chemistry letters,
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
October 2022,
Antibiotics (Basel, Switzerland),
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
November 2012,
ChemMedChem,
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
February 2021,
Pathogens (Basel, Switzerland),
Mei Liu, and
Prapon Wilairat, and
Simon L Croft, and
Agnes Lay-Choo Tan, and
Mei-Lin Go
April 1999,
Planta medica,
