8‐Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual‐Stage Antiplasmodial Activity

Abstract

A series of novel 8‐aminoquinolines (8‐AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8‐AQs bearing 2‐alkoxy and 5‐phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity.

Investigation of the mechanism of action of mefloquine and derivatives against the parasite Echinococcus multilocularis

“…These bioactive quinoline-based compounds were the precursors of several derivatives that are now used clinically and contribute greatly to the control of serious diseases worldwide ( Narwal et al, 2017 ; Sharma et al, 2017 ; Shang et al, 2018 ; Kucharski et al, 2022 ). In addition, several other compounds with quinoline nuclei fused or unfused to other heterocyclic compounds have been synthesized recently, exhibiting a wide range of biological properties in vitro and in vivo , such as antimalarials ( Leven et al, 2019 ), antifungals ( Shruthi et al, 2019 ), anticancer agents ( Hamdy et al, 2019 ), anticonvulsants ( Kumar and Abdullah, 2019 ), antihypertensives ( Vellalacheruvu et al, 2017 ), anti-inflammatories ( Deaton et al, 2019 ), antidepressants ( Galambos et al, 2017 ), and antivirals ( Kos et al, 2019 ).…”

Nanocatalyzed Synthetic Approach for the Quinazolinone and Quinazoline Derivatives: A Review (2015 – Present)

“…The biotransformation of terminal amino groups into hazardous aldehydes is a shared drawback of these molecules. The synthesis of novel compounds with aminoxy and oxime-groups was done to stop this change and to preserve good antimalarial activity 22 .…”

Quinolines and Quinolones as Antibacterial, Antifungal, Anti-virulence, Antiviral and Anti-parasitic Agents

“…Shared common disadvantage of these compounds is biotransformation of terminal amino-groups into aldehydes, which are toxic. To prevent such transformation and to maintain good antimalarial activity a new derivatives that contained aminoxy and oxime-groups were synthetized (Leven et al 2019). The compounds were evaluated in vitro against asexual blood stages, liver stages, and sexual stages of P. falciparum.…”