Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Ishmail, Fatima-Zahra, once mentioned the application of 90-52-8, Category: quinolines-derivatives, Name is 8-Amino-6-methoxyquinoline, molecular formula is C10H10N2O, molecular weight is 174.1992, MDL number is MFCD00672902, category is quinoxaline. Now introduce a scientific discovery about this category.
Diversification of quinoline-triazole scaffolds with CORMs: Synthesis, in vitro and in silico biological evaluation against Plasmodium falciparum
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. Of significance, the complexes retain their activity in the MDR strain with resistance indices ranging between 1.1 and 2.1. The Mn(I) analogues display photodissociation of all three CO ligands upon irradiation at 365 nm. More importantly, the complexes show increased antimalarial activity in vitro upon photoactivation, something not observed by the clinically used reference drug, chloroquine. As a purported mechanism of action, the compounds were evaluated as beta-haematin inhibitors. To further understand the interactions of the complexes, in silico hemozoin docking simulations were performed, attesting to the fact that CO-release could be vital for blocking the hemozoin formation pathway. These results show that this strategy may be a valuable, novel route to design antimalarial agents with higher efficacy.
If you are hungry for even more, make sure to check my other article about 90-52-8, Category: quinolines-derivatives.
Reference:
Quinoline – Wikipedia,
,Quinoline | C9H7N – PubChem