Insights into Structural and Physicochemical Properties Required for β-hematin Inhibition of Privileged Triarylimidazoles

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2021 Jan 22

PMID 33479606

Citations 2

Authors

Clinton G L Veale

Janeeka Jayram

Shivani Naidoo

Dustin Laming

Tarryn Swart

Tania Olivier

Matthew P Akerman

Katherine A de Villiers

Heinrich C Hoppe

Vineet Jeena

Affiliations

Soon will be listed here.

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, adsorption analysis indicated that these compounds exert their effect by inhibiting β-hematin crystal growth at the fast growing 001 face.

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