Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1)
Тип публикации: Journal Article
Дата публикации: 2013-05-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
23570789
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
A series of imidazopyridazines which are potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 ( Pf CDPK1) was identified from a high-throughput screen against the isolated enzyme. Subsequent exploration of the SAR and optimisation has yielded leading members which show promising in vitro anti-parasite activity along with good in vitro ADME and selectivity against human kinases. Initial in vivo testing has revealed good oral bioavailability in a mouse PK study and modest in vivo efficacy in a Plasmodium berghei mouse model of malaria.
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51
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51
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(1.96%)
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ГОСТ
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Chapman T. et al. Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) // Bioorganic and Medicinal Chemistry Letters. 2013. Vol. 23. No. 10. pp. 3064-3069.
ГОСТ со всеми авторами (до 50)
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Chapman T., Osborne S. A., Bouloc N., Large J. M., Wallace C., Birchall K., Ansell K. H., Jones H. E., Taylor D., Clough B., Green J., Holder A. A. Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) // Bioorganic and Medicinal Chemistry Letters. 2013. Vol. 23. No. 10. pp. 3064-3069.
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TY - JOUR
DO - 10.1016/j.bmcl.2013.03.017
UR - https://doi.org/10.1016/j.bmcl.2013.03.017
TI - Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1)
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Chapman, T
AU - Osborne, Simon A
AU - Bouloc, Nathalie
AU - Large, Jonathan M.
AU - Wallace, Claire
AU - Birchall, Kristian
AU - Ansell, Keith H
AU - Jones, Hayley E.
AU - Taylor, Debra
AU - Clough, Barbara
AU - Green, Judith
AU - Holder, Anthony A.
PY - 2013
DA - 2013/05/01
PB - Elsevier
SP - 3064-3069
IS - 10
VL - 23
PMID - 23570789
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (до 50 авторов)
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@article{2013_Chapman,
author = {T Chapman and Simon A Osborne and Nathalie Bouloc and Jonathan M. Large and Claire Wallace and Kristian Birchall and Keith H Ansell and Hayley E. Jones and Debra Taylor and Barbara Clough and Judith Green and Anthony A. Holder},
title = {Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1)},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2013},
volume = {23},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/j.bmcl.2013.03.017},
number = {10},
pages = {3064--3069},
doi = {10.1016/j.bmcl.2013.03.017}
}
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MLA
Скопировать
Chapman, T., et al. “Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).” Bioorganic and Medicinal Chemistry Letters, vol. 23, no. 10, May. 2013, pp. 3064-3069. https://doi.org/10.1016/j.bmcl.2013.03.017.