Synthesis and Antimalarial Activity Evaluation of Some Mannich Bases of Tetraoxane-Phenol Conjugate
1, 1, 1, 1
- 1Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, INDIA.
CORRESPONDENCE
Rudrapal Mithun
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, INDIA.
Received: 12-05-2016; Accepted: 19-09-2016.
Volume 50, Issue 4 · pp. 591-598 · 2016 · DOI: 10.5530/ijper.50.4.11
ABSTRACT
A new series of seven Mannich bases of tetraoxane-phenol conjugate as possible antimalarial compounds were synthesized and evaluated in vitro for their antimalarial activity. All the synthesized compounds exhibited good antimalarial activity against the CQ-sensitive strain (RKL-2) of P. falciparum. Compounds with 3-indolyl and phenolic substituent’s showed considerably superior activity than rest of the synthesized tetraoxane derivatives in the series, with IC50 values 8.19 μg/ml and 5.30 μg/ml, respectively. The activity was, however, less than that of the standard reference drug, CQ (IC50 0.04 μg/ml). Three selected compounds were also screened for the activity against a CQresistant strain (RKL-9) of P. falciparum, which was also found good with IC50 values 41.77 μg/ml, 39.87 μg/ml and 34.59 μg/ml for compounds having phenyl, furan-2-yl and 4-pyridyl substituent’s, respectively in the Mannich base component of the conjugated tetraoxane-phenol scaffold. The activity against CQ-sensitive strain of P. falciparum was better as compared to the activity seen against resistant strain. Results clearly indicate that Mannich bases of tetraoxane-phenol conjugate with bulky aromatic/heteroaromatic groups possess antimalarial potential both against CQ-sensitive and –resistant strains of P. falciparum.
KEYWORDS
REFERENCES
As publishedShowing references and in-text citations exactly as published.
Cite this article
SELECT FORMAT
Jinky, G., Dipak, C., Mukesh, K. K., & Mithun, R. (2016). Synthesis and Antimalarial Activity Evaluation of Some Mannich Bases of Tetraoxane-Phenol Conjugate. Indian Journal of Pharmaceutical Education and Research, 50(4), 591-598. https://doi.org/10.5530/ijper.50.4.11
Copyright and licence
© 2016 Author(s)
This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 License, which permits unrestricted use, distribution and reproduction in any medium, provided the original author and source are credited. CC BY 4.0