Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

[Image: see text] N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target...

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Autores principales: Bayliss, Tracy, Robinson, David A., Smith, Victoria C., Brand, Stephen, McElroy, Stuart P., Torrie, Leah S., Mpamhanga, Chido, Norval, Suzanne, Stojanovski, Laste, Brenk, Ruth, Frearson, Julie A., Read, Kevin D., Gilbert, Ian H., Wyatt, Paul G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734605/
https://www.ncbi.nlm.nih.gov/pubmed/29125744
http://dx.doi.org/10.1021/acs.jmedchem.7b01255
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author Bayliss, Tracy
Robinson, David A.
Smith, Victoria C.
Brand, Stephen
McElroy, Stuart P.
Torrie, Leah S.
Mpamhanga, Chido
Norval, Suzanne
Stojanovski, Laste
Brenk, Ruth
Frearson, Julie A.
Read, Kevin D.
Gilbert, Ian H.
Wyatt, Paul G.
author_facet Bayliss, Tracy
Robinson, David A.
Smith, Victoria C.
Brand, Stephen
McElroy, Stuart P.
Torrie, Leah S.
Mpamhanga, Chido
Norval, Suzanne
Stojanovski, Laste
Brenk, Ruth
Frearson, Julie A.
Read, Kevin D.
Gilbert, Ian H.
Wyatt, Paul G.
author_sort Bayliss, Tracy
collection PubMed
description [Image: see text] N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a starting point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT.
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spelling pubmed-57346052017-12-19 Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors Bayliss, Tracy Robinson, David A. Smith, Victoria C. Brand, Stephen McElroy, Stuart P. Torrie, Leah S. Mpamhanga, Chido Norval, Suzanne Stojanovski, Laste Brenk, Ruth Frearson, Julie A. Read, Kevin D. Gilbert, Ian H. Wyatt, Paul G. J Med Chem [Image: see text] N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a starting point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT. American Chemical Society 2017-11-10 2017-12-14 /pmc/articles/PMC5734605/ /pubmed/29125744 http://dx.doi.org/10.1021/acs.jmedchem.7b01255 Text en Copyright © 2017 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Bayliss, Tracy
Robinson, David A.
Smith, Victoria C.
Brand, Stephen
McElroy, Stuart P.
Torrie, Leah S.
Mpamhanga, Chido
Norval, Suzanne
Stojanovski, Laste
Brenk, Ruth
Frearson, Julie A.
Read, Kevin D.
Gilbert, Ian H.
Wyatt, Paul G.
Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title_full Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title_fullStr Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title_full_unstemmed Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title_short Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
title_sort design and synthesis of brain penetrant trypanocidal n-myristoyltransferase inhibitors
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734605/
https://www.ncbi.nlm.nih.gov/pubmed/29125744
http://dx.doi.org/10.1021/acs.jmedchem.7b01255
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