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

Bioorganic & Medicinal Chemistry Letters
A ParthibanH Surya Prakash Rao

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 f...Continue Reading

References

Feb 8, 2002·Nature·Brian Greenwood, Theonest Mutabingwa
Feb 8, 2002·Nature·Jeffrey Sachs, Pia Malaney
Mar 12, 2009·Current Drug Targets·Antoniana U KrettliLuisa G Krettli
Feb 1, 2009·Expert Opinion on Drug Discovery·Antoniana Ursine Krettli
Jul 26, 2014·European Journal of Medicinal Chemistry· NishaVipan Kumar

❮ Previous
Next ❯

Citations

Apr 6, 2016·Journal of Nanobiotechnology·Shadab AlamVirander Singh Chauhan
Jan 11, 2020·Journal of Biomolecular Structure & Dynamics·Zhe DuHong-Lin Zhai
Oct 31, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Seong-Min LeeDongyun Shin
Jan 28, 2020·Current Topics in Medicinal Chemistry·Mukesh C Joshi, Timothy J Egan
Sep 17, 2019·European Journal of Medicinal Chemistry·Anudeep K NarulaLalit M Nainwal

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antimalarial Agents (ASM)

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.

Antimalarial Agents

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.