Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles

Tukulula, Matshawandile; Louw, Stefan; Njoroge, Mathew; Chibale, Kelly

Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles

Journal Article

2020-12-15

Journal Title

Molecules

Link to Journal

https://www.mdpi.com/journal/molecules

Department

Department of Chemistry

Faculty

Faculty of Science

License

http://creativecommons.org/licenses/by/4.0/

Abstract

A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a–g) displayed good antiplasmodium activities (IC50 = 0.20–0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (200 µM) at pH 7.

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