Synthesis, antimalarial activity evaluation and molecular docking studies of some novel dispiro-1,2,4,5-tetraoxanes

Authors

  • Mukesh Kumar Kumawat Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam
  • Dipak Chetia Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam

DOI:

https://doi.org/10.3329/bjp.v10i4.24532

Keywords:

Antimalarial, Dispiro-1, 2, 4, 5-tetraoxane, Molecular docking

Abstract

Seven novel dispiro-1,2,4,5-tetraoxane derivatives were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were subsequently screened for in vitro antimalarial activity against chloroquine resistant strain of Plasmodium falciparum (RKL-9). At antimalarial activity screening, two compounds, namely 5d (MIC = 15.6 µg/mL or 64.5 µM) and 5f (MIC = 15.6 µg/mL or 54.6 µM) were found to be about 1.5 times more potent against chloroquine resistant strain-RKL-9 compared to chloroquine (MIC = 25.0 µg/mL or 78.3 µM). Molecular docking studies of potent ligands were also performed in cysteine protease binding pocket residues of falcipain-2 as a target protein.

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Published

2015-11-05

How to Cite

Kumawat, M. K., and D. Chetia. “Synthesis, Antimalarial Activity Evaluation and Molecular Docking Studies of Some Novel Dispiro-1,2,4,5-Tetraoxanes”. Bangladesh Journal of Pharmacology, vol. 10, no. 4, Nov. 2015, pp. 917-23, doi:10.3329/bjp.v10i4.24532.

Issue

Section

Research Articles