4.7 Article

Emergence of pyrido quinoxalines as new family of antimalarial agents

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 77, 期 -, 页码 280-287

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.010

关键词

Quinolones; Pyrido quinoxaline; Gould-Jacobs reaction; Antimalarial activity; Plasmodium falciparum

资金

  1. Council of Scientific and Industrial Research (CSIR-INDIA) through 12th five year plan project DITSF [CSC-0204]
  2. Department of Biotechnology and CSIR

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A series of novel N-alkyl dihydro pyrido quinoxaline derivatives were synthesized using Gould-Jacobs reaction and evaluated their antimalarial activity in vitro against chloroquine sensitive (3D7) and drug resistant (Dd2) strains of Plasmodium falciparum. Among the compounds tested, 10 compounds were more potent than their structural standard analog ciprofloxacin, including 2 derivatives 5e and 5h, which showed 3.3-7.4 times more potency than ciprofloxacin against both the parasite strains. The results are encouraging and a lead molecule may emerge which is useful alone or in combination therapy. (C) 2014 Elsevier Masson SAS. All rights reserved.

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