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Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles

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Abstract

In this study, we investigated a series of triarylimidazoles, in an effort to elucidate critical SAR information pertaining to their anti-plasmodial and β-hematin inhibitory activity. Our results showed that in addition to the positional effects of ring substitution, subtle changes to lipophilicity and imidazole ionisability were important factors in SAR interpretation. Finally, in silico adsorption analysis indicated that these compounds exert their effect by inhibiting β-hematin crystal growth at the fast growing 001 face.

Graphical abstract: Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles

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Article information


Submitted
03 Oct 2019
Accepted
22 Oct 2019
First published
16 Dec 2019

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles

C. G. L. Veale, J. Jayram, S. Naidoo, D. Laming, T. Swart, T. Olivier, M. P. Akerman, K. A. de Villiers, H. C. Hoppe and V. Jeena, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00468H

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