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Not Open Access | Diversification of quinoline-triazole scaffolds with CORMs: Synthesis, in vitro and in silico biological evaluation against Plasmodium falciparum

February 3, 2021 - 14:31 -- NOT Open Access
Ishmail FZ, Melis DR, Mbaba M, Smith GS
J Inorg Biochem. 2021 Feb;215:111328

A discrete series of tricarbonyl manganese and rhenium complexes conjugated to a quinoline-triazole hybrid scaffold were synthesised and their inhibitory activities evaluated against Plasmodium falciparum. In general, the complexes show moderate activity with improved inhibitory activities for the photoactivatable manganese(I) tricarbonyl complexes in the malaria parasite. All complexes are active in the dark against the NF54 CQS (chloroquine-sensitive) and K1 MDR (multidrug-resistant) strains of Plasmodium falciparum, with IC50 values in the low micromolar range.

NOT Open Access | A Diverse Range of Hemozoin Inhibiting Scaffolds Act on Plasmodium falciparum as Heme Complexes

January 12, 2021 - 14:30 -- NOT Open Access
Openshaw R, Maepa K, Benjamin SJ, Wainwright L, Combrinck JM, Hunter R, Egan TJ
ACS Infect Dis. 2021 Jan 12

A diverse series of hemozoin-inhibiting quinolines, benzamides, triarylimidazoles, quinazolines, benzimidazoles, benzoxazoles, and benzothiazoles have been found to lead to exchangeable heme levels in cultured Plasmodium falciparum (NF54) that ranged over an order of magnitude at the IC50. Surprisingly, less active compounds often exhibited higher levels of exchangeable heme than more active ones.

NOT Open Access | Identification of a novel binding mechanism of Quinoline based molecules with lactate dehydrogenase of Plasmodium falciparum

January 6, 2021 - 13:04 -- NOT Open Access
Singh R, Bhardwaj V, Purohit R
J Biomol Struct Dyn. 2021 Jan;39(1):348-356

The deadliest disease caused by the Plasmodium species is malaria. Among other species, the infection caused by Plasmodium falciparum (Pf) is life-threatening. The biological function and three-dimensional structure of PfLDH and human LDH are very similar. Any treatment aiming to inhibit the PfLDH can also affect the activity of human LDH. This study aims to identify molecules that show high selectivity for PfLDH without having a profound effect on the activity of human LDH. In this study, 30 in-house synthesized Quinolines based molecules were docked with both PfLDH and human LDH. Based on molecular docking results, molecules 3j, 4b, 4h, 4m were showed selectivity towards PfLDH.

NOT Open Access | Comparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors

January 6, 2021 - 13:03 -- NOT Open Access
Silveira FF, de Souza JO, Pinheiro LCS, et al.
Eur J Med Chem. 2021 Jan 1;209:112941

In this work, we designed and synthesized 35 new triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives as P. falciparum inhibitors (3D7 strain). Thirty compounds exhibited anti-P. falciparum activity, with IC50 values ranging from 0.030 to 9.1 μM. The [1,2,4]triazolo[1,5-a]pyrimidine derivatives were more potent than the pyrazolo[1,5-a]pyrimidine and quinoline analogues. Compounds 20, 21, 23 and 24 were the most potent inhibitors, with IC50 values in the range of 0.030-0.086 μM and were equipotent to chloroquine. In addition, the compounds were selective, showing no cytotoxic activity against the human hepatoma cell line HepG2. All [1,2,4]triazolo[1,5-a]pyrimidine derivatives inhibited PfDHODH activity in the low micromolar to low nanomolar range (IC50 values of 0.08-1.3 μM) and did not show significant inhibition against the HsDHODH homologue (0-30% at 50 μM).

Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria

May 14, 2020 - 12:18 -- Open Access
Liebman KM, Burgess SJ, Gunsaru B, Kelly JX, Li Y, Morrill W, Liebman MC, Peyton DH
Molecules. 2020 May 10;25(9). pii: E2251

Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history of modern drug development. Although much progress has been made in the search for novel antimalarial scaffolds, it may be that quinolines will remain useful, especially if very potent compounds from this class are discovered.

Mode of action of quinoline antimalarial drugs in red blood cells infected by Plasmodium falciparum revealed in vivo

November 18, 2019 - 16:15 -- Open Access
Sergey Kapishnikov, Trine Staalsø, Yang Yang, Jiwoong Lee, Ana J. Pérez-Berná, Eva Pereiro, Yang Yang, Stephan Werner, Peter Guttmann, Leslie Leiserowitz, and Jens Als-Nielsen
PNAS November 12, 2019 116 (46) 22946-22952

The most widely used antimalarial drugs belong to the quinoline family. Their mode of action has not been characterized at the molecular level in vivo. We report the in vivo mode of action of a bromo analog of the drug chloroquine in rapidly frozen Plasmodium falciparum-infected red blood cells.

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