Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design, Synthesis and In Vitro Antimalarial Evaluation of New Quinolinylhydrazone Derivatives

Author(s): Le Thi Thuy, Hoang Xuan Tien, Vu Dinh Hoang, Tran Khac Vu.

Abstract:

A series of novel quinolinylhydrazones (5a-f) was synthesized by the condensation reaction of 2,6-diarylsubstituted piperidin-4-ones (4a-f) with 7-chloro-4-hydrazinoquinoline (2). Novel quinolinylhydrazones containing Shiff bases 8a-f and 11a-f were obtained via the condensation of Shiff bases 7a-f and 10a-f with 7-chloro-4-hydrazinoquinoline. These synthesized hydrazones were screened for their in vitro antimalarial activities to chloroquine - sensitive (T96) and chloroquine – resistant (K1) strains of P.falciparum. Among the synthesized compounds, 11a exhibited strong antimalarial activity at IC50 of 103.4 ng/mL and 18.76 ng/mL to both strains of P.falciparum, respectively.

Keywords: Amodiaquine, Chloroquine, Hydrazone, Malarial, Plasmodium falciparum, Quinoline, asexual erythrocytic phase, erythrocyte ferritin, haemoglobin, nitroisoquinolines, piperidinyl moiety, Schiff bases, chloroquine-resistant strains, quinolinylhydrazone, piperidine nucleus, antimalarial potency

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Article Details

VOLUME: 9
ISSUE: 2
Year: 2012
Page: [163 - 168]
Pages: 6
DOI: 10.2174/157018012799079815
Price: $58