Design, Synthesis and Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials
Adimulam Chandra Shekhar,
Boddupally Pedda Venkat Lingaiah,
Pamulaparthy Shanthan Rao,
Aparna Devi Allanki,
Puran Singh Sijwali.
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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