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

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

Volume: 12 Issue: 5

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

Affiliation:

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

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.

Cite this article as:

Chandra Shekhar Adimulam, Pedda Venkat Lingaiah Boddupally, Shanthan Rao Pamulaparthy, Narsaiah Banda, Devi Allanki Aparna and Sijwali Puran Singh, Design, Synthesis and Biological Evaluation of Novel Fluorinated Heterocyclic Hybrid Molecules Based on Triazole & Quinoxaline Scaffolds Lead to Highly Potent Antimalarials and Antibacterials, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141111235301