Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 20, Pages 4657-4663Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.08.030
Keywords
Chloroquinoline-4H-chromene conjugates; In vitro antimalarial activity; In silico analysis
Categories
Funding
- Pondicherry University
- UCIBIO [UID/Multi/04378/2013]
- Fundacao para a Ciencia e a Tecnologia (FCT) Portugal [PTDC/QUI-BIQ/117799/2010, SFRH/BPD/97719/2013]
- Department of Biotechnology and Department of Information Technology, New Delhi, India
- UGC
- Department of Science and Technology (DST)
- Fundação para a Ciência e a Tecnologia [PTDC/QUI-BIQ/117799/2010] Funding Source: FCT
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A new series of chloroquinoline-4H-chromene conjugates incorporating piperizine or azipane tethers were synthesized and their anti-malarial activity were evaluated against two Plasmodium falciparum strains namely 3D7 chloroquine sensitive (CQS) and K1 chloroquine resistant (CQR). Chloroquine was used as the standard and also reference for comparison. The conjugates exhibit intense UV absorption with lambda(max) located at 342 nm (log epsilon = 4.0), 254 nm (log epsilon = 4.2), 223 nm (log epsilon = 4.4) which can be used to spectrometrically track the molecules even in trace amounts. Among all the synthetic compounds, two molecules namely 6-nitro and N-piperazine groups incorporated 7d and 6-chloro and N-azapane incorporated 15b chloroquinoline-4H-chromene conjugates showed significant anti-malarial activity against two strains (3D7 and K1) of P. falciparum. These values are lesser than the values of standard antimalarial compound. Molecular docking results suggested that these two compounds showing strong binding affinity with P. falciparum lactate dehydrogenase (PfLDH) and also they occupy the co-factor position which indicated that they could be the potent inhibitors for dreadful disease malaria and specifically attack the glycolytic pathway in parasite for energy production. (C) 2015 Elsevier Ltd. All rights reserved.
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