4.7 Article

Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 2, Pages 625-633

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.11.062

Keywords

Tetrahydropyridines; Antimalarial activity; L-Proline; Organocatalysis; Schizont maturation; Trifluoroacetic acid

Funding

  1. ICMR
  2. DBT New Delhi
  3. CSIR New Delhi [7466]

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A highly atom economic one pot synthesis of tetrahydropyridines was achieved by L-proline/TFA catalysed multicomponent reaction of beta-keto-esters, aromatic aldehydes and anilines. The synthesized compounds were screened against Plasmodium falciparum in vitro and one of them showed antimalarial activity with MIC as low as 0.09 mu g/mL. (C) 2008 Elsevier Ltd. All rights reserved.

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