(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Тип публикации: Journal Article
Дата публикации: 2004-12-13
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.1
Impact factor: 7.3
ISSN: 00222623, 15204804
PubMed ID:
15634008
Drug Discovery
Molecular Medicine
Краткое описание
A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC(50) = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo efficacy in animal models. MK-0431, the phosphate salt of compound 1, was selected for development as a potential new treatment for type 2 diabetes.
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Kim D. et al. (2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes // Journal of Medicinal Chemistry. 2004. Vol. 48. No. 1. pp. 141-151.
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Kim D., Wang L., Beconi M., Eiermann G. J., Fisher M. H., He H., Hickey G. J., Kowalchick J. E., LEITING B., Lyons K., Marsilio F., McCann M. E., PATEL R. A., Petrov A., Scapin G., Patel S. B., Roy R. S., WU J. K., Wyvratt M. J., Zhang B. B., Lan Z., THORNBERRY N. A., Weber A. E. (2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes // Journal of Medicinal Chemistry. 2004. Vol. 48. No. 1. pp. 141-151.
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TY - JOUR
DO - 10.1021/jm0493156
UR - https://doi.org/10.1021/jm0493156
TI - (2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
T2 - Journal of Medicinal Chemistry
AU - Kim, Dooseop
AU - Wang, Liping
AU - Beconi, Maria
AU - Eiermann, George J.
AU - Fisher, Michael H.
AU - He, Huaibing
AU - Hickey, Gerard J.
AU - Kowalchick, Jennifer E
AU - LEITING, Barbara
AU - Lyons, Kathryn
AU - Marsilio, Frank
AU - McCann, Margaret E.
AU - PATEL, Reshma A.
AU - Petrov, Aleksandr
AU - Scapin, Giovanna
AU - Patel, Sangita B
AU - Roy, Ranabir Sinha
AU - WU, Joseph K.
AU - Wyvratt, Matthew J.
AU - Zhang, Bei B.
AU - Lan, Zhu
AU - THORNBERRY, Nancy A.
AU - Weber, Ann E.
PY - 2004
DA - 2004/12/13
PB - American Chemical Society (ACS)
SP - 141-151
IS - 1
VL - 48
PMID - 15634008
SN - 0022-2623
SN - 1520-4804
ER -
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@article{2004_Kim,
author = {Dooseop Kim and Liping Wang and Maria Beconi and George J. Eiermann and Michael H. Fisher and Huaibing He and Gerard J. Hickey and Jennifer E Kowalchick and Barbara LEITING and Kathryn Lyons and Frank Marsilio and Margaret E. McCann and Reshma A. PATEL and Aleksandr Petrov and Giovanna Scapin and Sangita B Patel and Ranabir Sinha Roy and Joseph K. WU and Matthew J. Wyvratt and Bei B. Zhang and Zhu Lan and Nancy A. THORNBERRY and Ann E. Weber},
title = {(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes},
journal = {Journal of Medicinal Chemistry},
year = {2004},
volume = {48},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/jm0493156},
number = {1},
pages = {141--151},
doi = {10.1021/jm0493156}
}
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Kim, Dooseop, et al. “(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes.” Journal of Medicinal Chemistry, vol. 48, no. 1, Dec. 2004, pp. 141-151. https://doi.org/10.1021/jm0493156.
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