Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist

Yanping Xu; Daniel Mayhugh; Ashraf Saeed; Xiaodong Wang; Richard C. Thompson; Samuel J. Dominianni; Raymond F. Kauffman; Jaipal Singh; James S. Bean; William R. Bensch; Robert J. Barr; John Osborne; Chahrzad Montrose-Rafizadeh; Richard W. Zink; Nathan P. Yumibe; Naijia Huang; Debra Luffer-Atlas; Deepa Rungta; Dale E. Maise; Nathan B. Mantlo

doi:10.1021/jm034173l

Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist

Yanping Xu, Daniel Mayhugh, Ashraf Saeed, Xiaodong Wang, Richard C. Thompson, Samuel J. Dominianni, Raymond F. Kauffman, Jaipal Singh, James S. Bean, William R. Bensch, Robert J. Barr, John Osborne, Chahrzad Montrose-Rafizadeh, Richard W. Zink, Nathan P. Yumibe, Naijia Huang, Debra Luffer-Atlas, Deepa Rungta, Dale E. Maise, Nathan B. Mantlo

Cellular & Integrative Physiology

Research output: Contribution to journal › Article

65 Scopus citations

Abstract

A new series of hPPARα agonists containing a 2,4-dihydro-3H-1,2,4-triazol-3-one (triazolone) core is described leading to the discovery of 5 (LY518674), a highly potent and selective PPARα agonist.

Original language	English (US)
Pages (from-to)	5121-5124
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	46
Issue number	24
DOIs	https://doi.org/10.1021/jm034173l
State	Published - Nov 20 2003

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm034173l

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Xu, Y., Mayhugh, D., Saeed, A., Wang, X., Thompson, R. C., Dominianni, S. J., Kauffman, R. F., Singh, J., Bean, J. S., Bensch, W. R., Barr, R. J., Osborne, J., Montrose-Rafizadeh, C., Zink, R. W., Yumibe, N. P., Huang, N., Luffer-Atlas, D., Rungta, D., Maise, D. E., & Mantlo, N. B. (2003). Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist. Journal of Medicinal Chemistry, 46(24), 5121-5124. https://doi.org/10.1021/jm034173l

Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist. / Xu, Yanping; Mayhugh, Daniel; Saeed, Ashraf; Wang, Xiaodong; Thompson, Richard C.; Dominianni, Samuel J.; Kauffman, Raymond F.; Singh, Jaipal; Bean, James S.; Bensch, William R.; Barr, Robert J.; Osborne, John; Montrose-Rafizadeh, Chahrzad; Zink, Richard W.; Yumibe, Nathan P.; Huang, Naijia; Luffer-Atlas, Debra; Rungta, Deepa; Maise, Dale E.; Mantlo, Nathan B.

In: Journal of Medicinal Chemistry, Vol. 46, No. 24, 20.11.2003, p. 5121-5124.

Research output: Contribution to journal › Article

Xu, Y, Mayhugh, D, Saeed, A, Wang, X, Thompson, RC, Dominianni, SJ, Kauffman, RF, Singh, J, Bean, JS, Bensch, WR, Barr, RJ, Osborne, J, Montrose-Rafizadeh, C, Zink, RW, Yumibe, NP, Huang, N, Luffer-Atlas, D, Rungta, D, Maise, DE & Mantlo, NB 2003, 'Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist', Journal of Medicinal Chemistry, vol. 46, no. 24, pp. 5121-5124. https://doi.org/10.1021/jm034173l

Xu, Yanping ; Mayhugh, Daniel ; Saeed, Ashraf ; Wang, Xiaodong ; Thompson, Richard C. ; Dominianni, Samuel J. ; Kauffman, Raymond F. ; Singh, Jaipal ; Bean, James S. ; Bensch, William R. ; Barr, Robert J. ; Osborne, John ; Montrose-Rafizadeh, Chahrzad ; Zink, Richard W. ; Yumibe, Nathan P. ; Huang, Naijia ; Luffer-Atlas, Debra ; Rungta, Deepa ; Maise, Dale E. ; Mantlo, Nathan B. / Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist. In: Journal of Medicinal Chemistry. 2003 ; Vol. 46, No. 24. pp. 5121-5124.

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abstract = "A new series of hPPARα agonists containing a 2,4-dihydro-3H-1,2,4-triazol-3-one (triazolone) core is described leading to the discovery of 5 (LY518674), a highly potent and selective PPARα agonist.",

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AU - Thompson, Richard C.

AU - Dominianni, Samuel J.

AU - Kauffman, Raymond F.

AU - Singh, Jaipal

AU - Bean, James S.

AU - Bensch, William R.

AU - Barr, Robert J.

AU - Osborne, John

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AU - Luffer-Atlas, Debra

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AU - Maise, Dale E.

AU - Mantlo, Nathan B.

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