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 Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials

Author(s): Adimulam Chandra Shekhar, Boddupally Pedda Venkat Lingaiah, Pamulaparthy Shanthan Rao, Banda Narsaiah, Aparna Devi Allanki, Puran Singh Sijwali.

Graphical Abstract:


Abstract:

A series of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffold were designed, synthesized and evaluated for inhibition of Plasmodium falciparum, a virulent human malaria parasite. Mono and bis triazole tagged quinoxaline analogs were synthesized by propargylation of 6-amino quinoxaline followed by click reaction with various substituted aromatic azides under uncertain reaction conditions. The newly synthesized molecules were assessed for antimalarial activity and three of the analogs were identified as promising leads which killed parasites with IC50 values <10 μM and showed 27-70 selective indices.

Keywords: Antimalarials, click reaction, hybrid molecules, plasmodium, quinoxalines, triazoles.

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Article Details

VOLUME: 12
ISSUE: 5
Year: 2015
Page: [393 - 407]
Pages: 15
DOI: 10.2174/1570180812666141111235301
Price: $58