Abstract
A new series of compounds was prepared from 6-methoxyquinolin-8-amine or its N-(2-aminoethyl) analogue via Ugi-azide reaction. Their linkers between the quinoline and the tert-butyltetrazole moieties differ in chain length, basicity and substitution. Compounds were tested for their antiplasmodial activity against Plasmodium falciparum NF54 as well as their cytotoxicity against L-6-cells. The activity and the cytotoxicity were strongly influenced by the linker and its substitution. The most active compounds showed good activity and promising selectivity.
Highlights
Malaria, a vector-borne parasitic disease, is still one of the most dangerous infectious diseases worldwide
With more than 200 million cases in 2019 and 400.000 deaths malaria is a huge burden for mostly sub-Saharan African, South American, Southeast Asian countries [1]
As precursor for all final compounds served 6-methoxyquinolin-8-amine 2, which was synthesized in a two-step reaction from 4-methoxy-2-nitroaniline and glycerol in a so was synthesized in a two-step reaction from
Summary
A vector-borne parasitic disease, is still one of the most dangerous infectious diseases worldwide. Even against artemisinin derivatives, which are usually combined with other drugs in the first-line treatment of malaria, first resistances are emerging [3,4]. Because of the threat of potentially untreatable malaria infections new active compounds are urgently needed. Pandey et al published a series of compounds where a 4-aminochinoline moiety was linked with a tetrazole ring. In this case an aminophenyl motive functioned as a linker. These compounds possessed antimalarial activities in the submicromolar range. We published a series of 7-chloroquinoline derivatives that were linked with a tetrazole ring as well as different lipophilic aliphatic and aromatic side chains. A piperidine ring was as a linker instead ofaminophenyl the aminophenyl moiety.
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