Bioorganic and Medicinal Chemistry p. 6332 - 6344 (2017)
Update date:2022-09-26
Topics:
Tian, Junjun
Vandermosten, Leen
Peigneur, Steve
Moreels, Lien
Rozenski, Jef
Tytgat, Jan
Herdewijn, Piet
Van den Steen, Philippe E.
De Jonghe, Steven
Astemizole is a H1-antagonist endowed with antimalarial activity, but has hERG liabilities. Systematic structural modifications of astemizole led to the discovery of analogues that display very potent activity as inhibitors of the growth of the Plasmodium parasite, but show a decreased hERG inhibition, when compared to astemizole. These compounds can be used as starting point for the development of a new class of antimalarials.
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