Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis
Тип публикации: Journal Article
Дата публикации: 2003-09-27
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
14561098
Drug Discovery
Molecular Medicine
Краткое описание
3(S)-(6-methoxypyridin-3-yl)-3-[2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)propyl]imidazolidin-1-yl]propionic acid 6 was identified as a potent and selective antagonist of the alpha(v)beta(3) receptor. This compound has an excellent in vitro profile (IC(50) = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism.
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Hutchinson J. H. et al. Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis // Journal of Medicinal Chemistry. 2003. Vol. 46. No. 22. pp. 4790-4798.
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Hutchinson J. H., Halczenko W., Brashear K. M., Breslin M. J., Coleman P. J., DUONG L. T., Fernandez-Metzler C., Gentile M. A., FISHER J. E., Hartman G. W., Huff J. R., Kimmel D. L., Leu C., Meissner R. S., Merkle K., Nagy R., Pennypacker B., Perkins J. J., Prueksaritanont T., RODAN G. A., Varga S. L., Wesolowski G. A., Zartman A. E., Rodan S. B., Duggan M. E. Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis // Journal of Medicinal Chemistry. 2003. Vol. 46. No. 22. pp. 4790-4798.
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TY - JOUR
DO - 10.1021/jm030306r
UR - https://doi.org/10.1021/jm030306r
TI - Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis
T2 - Journal of Medicinal Chemistry
AU - Hutchinson, John H
AU - Halczenko, Wasyl
AU - Brashear, Karen M
AU - Breslin, Michael J
AU - Coleman, Paul J
AU - DUONG, LE T.
AU - Fernandez-Metzler, Carmen
AU - Gentile, Michael A
AU - FISHER, JOHN E.
AU - Hartman, George W.
AU - Huff, Joel R.
AU - Kimmel, D. L.
AU - Leu, Chih-Tai
AU - Meissner, Robert S
AU - Merkle, Kara
AU - Nagy, Rose
AU - Pennypacker, Brenda
AU - Perkins, James J
AU - Prueksaritanont, Thomayant
AU - RODAN, GIDEON A.
AU - Varga, Sandor L
AU - Wesolowski, Greg A
AU - Zartman, Amy E
AU - Rodan, Sevgi B.
AU - Duggan, Mark E.
PY - 2003
DA - 2003/09/27
PB - American Chemical Society (ACS)
SP - 4790-4798
IS - 22
VL - 46
PMID - 14561098
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2003_Hutchinson,
author = {John H Hutchinson and Wasyl Halczenko and Karen M Brashear and Michael J Breslin and Paul J Coleman and LE T. DUONG and Carmen Fernandez-Metzler and Michael A Gentile and JOHN E. FISHER and George W. Hartman and Joel R. Huff and D. L. Kimmel and Chih-Tai Leu and Robert S Meissner and Kara Merkle and Rose Nagy and Brenda Pennypacker and James J Perkins and Thomayant Prueksaritanont and GIDEON A. RODAN and Sandor L Varga and Greg A Wesolowski and Amy E Zartman and Sevgi B. Rodan and Mark E. Duggan},
title = {Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis},
journal = {Journal of Medicinal Chemistry},
year = {2003},
volume = {46},
publisher = {American Chemical Society (ACS)},
month = {sep},
url = {https://doi.org/10.1021/jm030306r},
number = {22},
pages = {4790--4798},
doi = {10.1021/jm030306r}
}
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MLA
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Hutchinson, John H., et al. “Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis.” Journal of Medicinal Chemistry, vol. 46, no. 22, Sep. 2003, pp. 4790-4798. https://doi.org/10.1021/jm030306r.