Synthesis of chromenochalcones and evaluation of their in vitro antileishmanial activity |
| |
Authors: | Narender Tadigoppula Khaliq Tanvir Shweta Nishi Goyal Neena Gupta Suman |
| |
Institution: | Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India. tnarender@rediffmail.com |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|