Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static-Cidal Screening of Analogues.

Animals Humans Trypanosomiasis, African / drug therapy Trypanocidal Agents / therapeutic use Cytostatic Agents / therapeutic use Trypanosoma brucei brucei Blood-Brain Barrier

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
13 07 2023
Historique:
medline: 14 7 2023
pubmed: 21 6 2023
entrez: 21 6 2023
Statut: ppublish

Résumé

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there is still a need for new drugs with eradication now a realistic possibility. Here, we report the development of 2,4-diaminothiazoles that demonstrate significant potency against

Identifiants

DOI: 10.1021/acs.jmedchem.3c00509 PMID: 37343180 PMC: PMC10350920
pubmed: 37343180
doi: 10.1021/acs.jmedchem.3c00509
pmc: PMC10350920
doi:

Substances chimiques

Trypanocidal Agents 0
Cytostatic Agents 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

8896-8916

Subventions

Organisme : Wellcome Trust
ID : 203134/Z/16/Z
Pays : United Kingdom
Organisme : Wellcome Trust
ID : WT083481
Pays : United Kingdom
Organisme : Wellcome Trust
ID : WT077705
Pays : United Kingdom
Organisme : Wellcome Trust
ID : 105021
Pays : United Kingdom
Organisme : Wellcome Trust
Pays : United Kingdom
Organisme : Wellcome Trust
ID : 218448/Z/19/Z
Pays : United Kingdom

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Auteurs

Laura A T Cleghorn (LAT)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Richard J Wall (RJ)

Wellcome Centre for Anti-infectives Research, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Sébastien Albrecht (S)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Stuart A MacGowan (SA)

Division of Computational Biology, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.
ORCID: 0000-0003-4233-5071

Suzanne Norval (S)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Manu De Rycker (M)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.
ORCID: 0000-0002-3171-3519

Andrew Woodland (A)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Daniel Spinks (D)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Stephen Thompson (S)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Stephen Patterson (S)

Wellcome Centre for Anti-infectives Research, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Victoriano Corpas Lopez (V)

Wellcome Centre for Anti-infectives Research, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Gourav Dey (G)

Wellcome Centre for Anti-infectives Research, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Iain T Collie (IT)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Irene Hallyburton (I)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Robert Kime (R)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Frederick R C Simeons (FRC)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Laste Stojanovski (L)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Julie A Frearson (JA)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Paul G Wyatt (PG)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.

Kevin D Read (KD)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.
ORCID: 0000-0002-8536-0130

Ian H Gilbert (IH)

Drug Discovery Unit, Wellcome Centre for Anti-infectives Research, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.
ORCID: 0000-0002-5238-1314

Susan Wyllie (S)

Wellcome Centre for Anti-infectives Research, School of Life Sciences, University of Dundee, Dow Street, Dundee DD1 5EH, U.K.
ORCID: 0000-0001-8810-5605

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Infection › Maladies vectorielles › Maladie du sommeil › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Trypanocides › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Actions chimiques et utilisations › Actions toxiques › Noxas › Cytostatiques › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Eucaryotes › Euglénozoaires › Kinetoplastida › Trypanosomatina › Trypanosoma › Trypanosoma brucei brucei › Development of a 2,4-Diaminothiazole Series...
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Barrière hémato-encéphalique › Development of a 2,4-Diaminothiazole Series...