Abstract
1H-3-{4-[(3-Dimethylaminopropyl)aminomethyl]phenyl}-2-phenylindole was synthesized via a multi-step pathway starting from 2-iodoaniline. Structure characterization of this new indole compound was achieved by 1H-NMR, 13C-NMR and ESI-MS spectral analysis. The title compound was screened in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani and Trypanosoma brucei brucei). Biological results showed antiparasitic activity with IC50 values in the μM range.
Highlights
Numerous indole-containing synthetic derivatives and natural products demonstrate pharmacological activities of importance to human disease
Available reagents were used as received without additional purification
Melting points were determined with an SM-LUX-POL Leitz hot-stage microscope (Leitz GMBH, Midland, ON, USA) and are uncorrected
Summary
Numerous indole-containing synthetic derivatives and natural products demonstrate pharmacological activities of importance to human disease. Indoles constitute the basis of an important class of compounds with interesting and promising biological activities [1,2,3,4,5] This nitrogen heterocyclic scaffold has gained much interest due to its wide range of biological activity upon modifications, including antiviral, antibacterial, anticancer, anti-Alzheimer’s disease and antiparasitic properties [6,7,8,9,10,11]. In this last field, the indole compounds are considered as attractive candidates for antiprotozoal therapy [11,12,13,14]. We report on the synthesis and structural identification of this new indole scaffold, which was screened in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani and Trypanosoma brucei brucei)
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