2024-03-29T08:34:03Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1784592020-10-06T08:15:41Zcom_10261_64com_10261_1col_10261_317
DIGITAL.CSIC
author
Klug, Dana M.
author
Díaz-González, Rosario
author
Pérez-Moreno, Guiomar
author
Ceballos-Pérez, Gloria
author
García-Hernández, Raquel
author
Gómez-Pérez, Veronica
author
Ruiz-Pérez, Luis Miguel
author
Rojas-Barros, Domingo I.
author
Gamarro, Francisco
author
González-Pacanowska, D.
author
Martínez-Martínez, María S.
author
Manzano, Pilar
author
Ferrins, Lori
author
Caffrey, Conor R.
author
Navarro, M.
author
Pollastri, M.P.
funder
National Institute of Allergy and Infectious Diseases (US)
funder
Ministerio de Economía, Industria y Competitividad (España)
funder
Junta de Andalucía
funder
Instituto de Salud Carlos III
orcid
Klug, Dana M. [0000-0002-8982-0640]
orcid
Gamarro, Francisco [0000-0003-1347-3440]
orcid
González-Pacanowska, D. [0000-0002-4303-5209]
orcid
Navarro, M. [0000-0003-2301-2699]
orcid
Pollastri, M.P. [0000-0001-9943-7197]
2019-03-25T11:51:36Z
2019-03-25T11:51:36Z
2019-02-08
PLoS Neglected Tropical Diseases
1935-2727
http://hdl.handle.net/10261/178459
10.1371/journal. pntd.0007129
1935-2735
http://dx.doi.org/10.13039/501100010198http://dx.doi.org/10.13039/100000060http://dx.doi.org/10.13039/501100004587http://dx.doi.org/10.13039/501100011011http://dx.doi.org/10.13039/100006492
New treatments are needed for neglected tropical diseases (NTDs) such as Human African
trypanosomiasis (HAT), Chagas disease, and schistosomiasis. Through a whole organism
high-throughput screening campaign, we previously identified 797 human kinase inhibitors
that grouped into 59 structural clusters and showed activity against T. brucei, the causative
agent of HAT. We herein report the results of further investigation of one of these clusters
consisting of substituted isatin derivatives, focusing on establishing structure-activity and
-property relationship scope. We also describe their in vitro absorption, distribution, metabolism, and excretion (ADME) properties. For one isatin, NEU-4391, which offered the best
activity-property profile, pharmacokinetic parameters were measured in mice.
eng
openAccess
Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents
artículo
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URL
https://digital.csic.es/bitstream/10261/178459/1/Klug-2019-Evaluation-of-a-class-of-isatinoids.pdf
File
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c39af2e008311345077f3312cff10389
1168010
application/pdf
Klug-2019-Evaluation-of-a-class-of-isatinoids.pdf