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Title: Experimental and computational evaluation of new quinolinyl chalcones as potent antiplasmodial agents
Authors: Dave, Shikha S
Ghatolea, Ajay M
Rahatgaonkar, Anjali M
Chorghade, Mukund S
Chauhan, P M S
Srivastava, Kumkum
Keywords: (<i style="">E</i>)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxyphenyl) prop-2-en-1-one
(<i style="">E</i>)-(2-chloro-6-ethoxyquinolin-3-yl) (2-hydroxyphenyl) prop-2-en-1-one
(<i style="">2Z</i>)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxyphenyl)-3-iodoprop-2-en-1-one
anti-malarial activity
Issue Date: Dec-2009
Publisher: CSIR
Abstract: <smarttagtype namespaceuri="urn:schemas-microsoft-com:office:smarttags" name="PersonName"> In a search for new antiplasmodial agents, a series of thirty five diversely substituted chalcones derived from a quinoline-chalcone scaffold e.g. (<i style="">E</i>)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxyphenyl) prop-2-en-1-one / (<i style="">E</i>)-(2-chloro-6-ethoxyquinolin-3-yl) (2-hydroxyphenyl) prop-2-en-1-one and (<i style="">2Z</i>)-3-(2-chloroquinolin-3-yl)-1-(2-hydroxyphenyl)-3-iodoprop-2-en-1-one are synthesized and studied. Compounds are prepared <i style="">via</i> Claisen–Schmidt condensations of 2-chloro-3-formyl quinoline / 2-chloro-6-ethoxy-3-formyl quinoline with appropriately substituted 2-hydroxy acetophenones. All compounds are assayed for their binding in the active sites of <i style="">Plasmodium falciparum</i> <i style="">lactate dehydrogenase</i> (pfLDH) enzyme. The quinoline chalcone derivatives showed negative binding energies promising potent pfLDH inhibitory activity. Compounds showing the highest negative binding scores have been studied for their <i style="">in vitro</i> antimalarial activity against cultured <i style="">Plasmodium falciparum 3D7 strain</i>. The compounds <b>2c</b> and <b>2u</b> have completely inhibited the maturation of parasites at MIC 10 µg/mL and above whereas <b>3b</b> inhibited 95% maturation of parasites at MIC 50 µg/mL. Additional efforts are being directed towards elaborating these leads towards the discovery and development of new quinolinyl heterocycles as anti-malarial agents. </smarttagtype>
Description: 1780-1793
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.48B(12) December 2009]

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