Synthesis and Antimalarial Activity Evaluation of Some Mannich Bases of Tetraoxane-Phenol Conjugate
Gogoi Jinky1, Chetia Dipak1, Kumawat Kumar Mukesh1, Rudrapal Mithun1
- 1Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, INDIA.
CORRESPONDENCE
Received: 12-05-2016; Revised: 31-08-2016; Accepted: 19-09-2016.
Volume 50, Issue 4 · pp. 591–598 · PUBLISHED 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 CQ resistant 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.
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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