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Bioorg Med Chem. 2005 Dec 1;13(23):6543-50. Epub 2005 Sep 26.

Synthesis of chromenochalcones and evaluation of their in vitro antileishmanial activity.

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Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India.


A large number of novel chromenochalcones were synthesized by pyridine-catalysed chromenylation of mono-chelated meta-dihydric acetophenones with the monoterpene, citral dimethyl acetal and subsequent Claisen-Schmidt condensation of the resultant acylchromenes with appropriate aromatic aldehydes. These chromenochalcones 1-19 were screened against in vitro extracellular promastigotes and intracellular amastigotes of Leishmania donovani. The most potent compound in this series was compound 9 with a pyridine ring-A, which showed 99% inhibition of promastigotes at 10 microg/ml, 82% at 0.25 microg/ml and 96% at 10 microg/ml concentration against amastigotes.

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