Abstract
The antiprotozoal activity of 1-benzyltetrahydropyridin-4-yliden iminium salts is reported. This paper describes the preparation of a series of analogs from dihydropyridines or dihydrothiopyrans as educts. The new compounds were investigated for their activity against Plasmodium falciparum NF54, a causative organism of Malaria tropica and Trypanosoma brucei rhodesiense, the causative organism of Human African Trypanosomiasis (sleeping sickness). Several structure–activity relationships were detected. Both the substituents in ring positions 1 and 4 of the tetrahydropyridinium moiety had a strong impact on the antiprotozoal activities as well as on the cytotoxicity of compounds against L-6 cells (rat skeletal myoblasts). All new compounds were characterized using FT-IR spectroscopy, HRMS, and NMR spectroscopy.Graphic abstract
Highlights
In 2019, an estimated 229 million cases of malaria, leading to estimated 409 000 deaths, occurred worldwide
This paper reports the synthesis of a series of new tetrahydropyridin-4-ylidene ammonium salts and their activities against Plasmodium falciparum NF54 and Trypanosoma brucei gambiense
A number of tetrahydropyridin-4-yliden iminiumsalts and a few related compounds have been prepared in several steps from dihydropyridines or dihydrothiopyrans as starting compounds
Summary
In 2019, an estimated 229 million cases of malaria, leading to estimated 409 000 deaths, occurred worldwide.
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