Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation
Тип публикации: Journal Article
Дата публикации: 2010-02-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
20097563
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
Efforts to refine the SAR of the piperazinyl-glutamate-pyridines for more potent analogs with improved pharmacokinetic profiles are described. Exploring substituted piperidines and other ring systems at the 4-pyridyl position led to compounds with improved potency and pharmacokinetic properties over candidate I. In particular, compounds 4t and 5t were discovered with a 10-fold improvement over potency and improved pharmacokinetic profiles in both the rat and dog.
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Parlow J. J. et al. Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 4. pp. 1388-1394.
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Parlow J. J., Burney M. W., Case B. L., Girard T. J., Hall K. A., Harris P., Hiebsch R. R., Huff R. M., Lachance R. M., Mischke D. A., Rapp S. R., Woerndle R. S., Ennis M. D. Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 4. pp. 1388-1394.
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TY - JOUR
DO - 10.1016/j.bmcl.2009.12.110
UR - https://doi.org/10.1016/j.bmcl.2009.12.110
TI - Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Parlow, John J.
AU - Burney, Mary W
AU - Case, Brenda L.
AU - Girard, Thomas J.
AU - Hall, Kerri A.
AU - Harris, Peter
AU - Hiebsch, Ronald R.
AU - Huff, Rita M.
AU - Lachance, Rhonda M.
AU - Mischke, Deborah A
AU - Rapp, Stephen R.
AU - Woerndle, Rhonda S
AU - Ennis, Michael D
PY - 2010
DA - 2010/02/01
PB - Elsevier
SP - 1388-1394
IS - 4
VL - 20
PMID - 20097563
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2010_Parlow,
author = {John J. Parlow and Mary W Burney and Brenda L. Case and Thomas J. Girard and Kerri A. Hall and Peter Harris and Ronald R. Hiebsch and Rita M. Huff and Rhonda M. Lachance and Deborah A Mischke and Stephen R. Rapp and Rhonda S Woerndle and Michael D Ennis},
title = {Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.bmcl.2009.12.110},
number = {4},
pages = {1388--1394},
doi = {10.1016/j.bmcl.2009.12.110}
}
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MLA
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Parlow, John J., et al. “Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 4, Feb. 2010, pp. 1388-1394. https://doi.org/10.1016/j.bmcl.2009.12.110.