Exploration of 3-methylisoquinoline-4-carbonitriles as Protein Kinase A inhibitors of Plasmodium Falciparum
| avondale-bepress.context-key | 9758971 | |
| avondale-bepress.submission-path | sci_math_papers/85 | |
| avondale.faculty | Science | |
| avondale.reporting.isPeerReviewed | Peer Reviewed | |
| avondale.reporting.version | Published Version | |
| dc.contributor.author | Abbott, Belinda M. | |
| dc.contributor.author | Wilson, David J. | |
| dc.contributor.author | Gilson, Paul R. | |
| dc.contributor.author | Crabb, Brendan S. | |
| dc.contributor.author | Prinz, Boris | |
| dc.contributor.author | Harvey, Katherine L. | |
| dc.contributor.author | Buskes, Melissa J. | |
| dc.date.accessioned | 2023-11-01T00:24:42Z | |
| dc.date.available | 2023-11-01T00:24:42Z | |
| dc.date.issued | 2016-06-01 | |
| dc.date.submitted | 2017-02-27T19:27:01Z | |
| dc.description.abstract | <p>A series of isoquinolines have been evaluated in a homology model of Plasmodium falciparum Protein Kinase A (PfPKA) using molecular dynamics. Synthesis of these compounds was then undertaken to investigate their structure–activity relationships. One compound was found to inhibit parasite growth in an in vitro assay and provides a lead to further develop 3-methylisoquinoline-4-carbonitriles as antimalarial compounds. Development of a potent and selective PfPKA inhibitor would provide a useful tool to shed further insight into the mechanisms enabling malaria parasites to establish infection.</p> | |
| dc.identifier.citation | <p>Buskes, M. J., Harvey, K. L., Prinz, B., Crabb, B. S., Gilson, P. R., Wilson, D. J., & Abbott, B. M. (2016). Exploration of 3-methylisoquinoline-4-carbonitriles as protein kinase A inhibitors of Plasmodium falciparum. <em>Bioorganic & Medicinal Chemistry, 24</em>(11), 2389-2396. doi:10.1016/j.bmc.2016.03.048</p> | |
| dc.identifier.doi | https://doi.org/10.1016/j.bmc.2016.03.048 | |
| dc.identifier.issn | 0968-0896 | |
| dc.identifier.uri | https://research.avondale.edu.au/handle/1897/09758971 | |
| dc.language.iso | en_us | |
| dc.provenance | <p>This article was originally published as:</p> <p>Buskes, M. J., Harvey, K. L., Prinz, B., Crabb, B. S., Gilson, P. R., Wilson, D. J., & Abbott, B. M. (2016). Exploration of 3-methylisoquinoline-4-carbonitriles as protein kinase A inhibitors of Plasmodium falciparum. <em>Bioorganic & Medicinal Chemistry, 24</em>(11), 2389-2396. doi: 10.1016/j.bmc.2016.03.048</p> <p>ISSN: 0968-0896</p> | |
| dc.relation.ispartof | Bioorganic & Medicinal Chemistry | |
| dc.rights | <p>Due to copyright restrictions this article is unavailable for download.</p> <p>Copyright © 2016 Published by Elsevier Ltd. All rights reserved.</p> <p>Staff and Students of Avondale College may access the full text of this article via Library PRIMO search <a href="https://avondale-primo.hosted.exlibrisgroup.com/primo-explore/search?vid=AVN&lang=en_US">here</a>.</p> | |
| dc.subject | Isoquinolines; Protein Kinase A; Antimalarials; Inhibitors | |
| dc.title | Exploration of 3-methylisoquinoline-4-carbonitriles as Protein Kinase A inhibitors of Plasmodium Falciparum | |
| dc.type | Journal Article |