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.
Reference:
Tukulula, M., Louw, S., Njoroge, M. & Chibale, K. 2020. Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. Molecules. 25(24) http://hdl.handle.net/11427/35234
Tukulula, M., Louw, S., Njoroge, M., & Chibale, K. (2020). Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. Molecules, 25(24), http://hdl.handle.net/11427/35234
Tukulula, Matshawandile, Stefan Louw, Mathew Njoroge, and Kelly Chibale "Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles." Molecules 25, 24. (2020) http://hdl.handle.net/11427/35234
Tukulula M, Louw S, Njoroge M, Chibale K. Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. Molecules. 2020;25(24) http://hdl.handle.net/11427/35234.
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