Lead Optimization of Dehydroemetine for Repositioned Use in Malaria-Reference-Cited by-同舟云学术

Lead Optimization of Dehydroemetine for Repositioned Use in Malaria

Published:2020-03-24 Issue:4 Volume:64 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Panwar Priyanka¹,Burusco Kepa K.²,Abubaker Muna¹,Matthews Holly³,Gutnov Andrey⁴,Fernández-Álvaro Elena⁵,Bryce Richard A.²,Wilkinson James¹,Nirmalan Niroshini¹

Affiliation:

1. Environment and Life Sciences, University of Salford, Greater Manchester, United Kingdom

2. Division of Pharmacy and Optometry, School of Health Sciences, Faculty of Biology, Medicine and Health, Manchester Academic Health Science Centre, University of Manchester, Manchester, United Kingdom

3. Keele University, Newcastle-under-Lyme, Staffordshire, United Kingdom

4. Chiroblock GMBH, Wolfen, Germany

5. GlaxoSmithKline, Diseases of the Developing World Medicines Development Campus, Tres Cantos, Spain

Abstract

Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel antimalarial treatments. The antiamoebic compound emetine dihydrochloride has been identified as a potent in vitro inhibitor of the multidrug-resistant strain K1 of Plasmodium falciparum (50% inhibitory concentration [IC 50 ], 47 nM ± 2.1 nM [mean ± standard deviation]). Dehydroemetine, a synthetic analogue of emetine dihydrochloride, has been reported to have less-cardiotoxic effects than emetine.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.01444-19

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