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Metallocene Antimalarials: The Continuing Quest
Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to...
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Formato: | Texto |
Lenguaje: | English |
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Hindawi Publishing Corporation
2008
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2225612/ https://www.ncbi.nlm.nih.gov/pubmed/18274662 http://dx.doi.org/10.1155/2008/495123 |
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author | Blackie, Margaret A. L. Chibale, Kelly |
author_facet | Blackie, Margaret A. L. Chibale, Kelly |
author_sort | Blackie, Margaret A. L. |
collection | PubMed |
description | Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine in order to develop a series of ferroquine derivatives. The replacement of the ferrocenyl moiety with ruthenocene has given rise to ruthenoquine and a modest series of analogues. The reaction of ferroquine and selected analogues with Au(PP [Formula: see text]) [Formula: see text] , Au([Formula: see text])(tht), and [Rh(COD) [Formula: see text]] has resulted in a series of heterobimetallic derivatives. In all cases, compounds have been evaluated for in vitro antiplasmodial activity in both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Preliminary structure-activity relationships have been delineated. |
format | Text |
id | pubmed-2225612 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2008 |
publisher | Hindawi Publishing Corporation |
record_format | MEDLINE/PubMed |
spelling | pubmed-22256122008-02-14 Metallocene Antimalarials: The Continuing Quest Blackie, Margaret A. L. Chibale, Kelly Met Based Drugs Review Article Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine in order to develop a series of ferroquine derivatives. The replacement of the ferrocenyl moiety with ruthenocene has given rise to ruthenoquine and a modest series of analogues. The reaction of ferroquine and selected analogues with Au(PP [Formula: see text]) [Formula: see text] , Au([Formula: see text])(tht), and [Rh(COD) [Formula: see text]] has resulted in a series of heterobimetallic derivatives. In all cases, compounds have been evaluated for in vitro antiplasmodial activity in both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Preliminary structure-activity relationships have been delineated. Hindawi Publishing Corporation 2008 2007-10-28 /pmc/articles/PMC2225612/ /pubmed/18274662 http://dx.doi.org/10.1155/2008/495123 Text en Copyright © 2008 M. A. L. Blackie and K. Chibale. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Review Article Blackie, Margaret A. L. Chibale, Kelly Metallocene Antimalarials: The Continuing Quest |
title | Metallocene Antimalarials: The Continuing Quest |
title_full | Metallocene Antimalarials: The Continuing Quest |
title_fullStr | Metallocene Antimalarials: The Continuing Quest |
title_full_unstemmed | Metallocene Antimalarials: The Continuing Quest |
title_short | Metallocene Antimalarials: The Continuing Quest |
title_sort | metallocene antimalarials: the continuing quest |
topic | Review Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2225612/ https://www.ncbi.nlm.nih.gov/pubmed/18274662 http://dx.doi.org/10.1155/2008/495123 |
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