2. Academic Validation
  3. Synthesis, in vitro and in silico antimalarial activity of 7-chloroquinoline and 4H-chromene conjugates

Synthesis, in vitro and in silico antimalarial activity of 7-chloroquinoline and 4H-chromene conjugates

  • Bioorg Med Chem Lett. 2015 Oct 15;25(20):4657-63. doi: 10.1016/j.bmcl.2015.08.030.
A Parthiban 1,  J Muthukumaran 2,  Ashan Manhas 3,  Kumkum Srivastava 4,  R Krishna 5,  H Surya Prakash Rao 6
Affiliations

Affiliations

  • 1 Department of Chemistry, School of Physical, Chemical and Applied Sciences, Pondicherry University, Puducherry 605 014, India.
  • 2 UCIBIO@REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal.
  • 3 Parasitology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
  • 4 Parasitology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India. Electronic address: kumkum_srivastava@cdri.res.in.
  • 5 Centre for Bioinformatics, School of Life Sciences, Pondicherry University, Puducherry 605 014, India. Electronic address: krishstrucbio@gmail.com.
  • 6 Department of Chemistry, School of Physical, Chemical and Applied Sciences, Pondicherry University, Puducherry 605 014, India. Electronic address: hspr.che@pondiuni.edu.in.
PMID: 26338359 DOI: 10.1016/j.bmcl.2015.08.030
Abstract

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 λmax located at 342 nm (log ε=4.0), 254 nm (log ε=4.2), 223 nm (log ε=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.

Keywords

Chloroquinoline-4H-chromene conjugates; In silico analysis; In vitro antimalarial activity.

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