| Literature DB >> 29042223 |
Junjun Tian1, Leen Vandermosten2, Steve Peigneur3, Lien Moreels3, Jef Rozenski1, Jan Tytgat3, Piet Herdewijn1, Philippe E Van den Steen2, Steven De Jonghe4.
Abstract
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.Entities:
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Year: 2017 PMID： 29042223 DOI： 10.1016/j.bmc.2017.10.004
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641