Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing

DOI: 10.1016/j.bmcl.2017.10.037

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 5230 - 5234 (2017)

Update date:2022-08-31

Topics:

Authors:

Lagu, Bharat

Kluge, Arthur F.

Fredenburg, Ross A.

Tozzo, Effie

Senaiar, Ramesh S.

Jaleel, Mahaboobi

Panigrahi, Sunil K.

Tiwari, Nirbhay K.

Krishnamurthy, Narasimha R.

Takahashi, Taisuke

Patane, Michael A.

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Article abstract of DOI:10.1016/j.bmcl.2017.10.037

Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.

Full text of DOI:10.1016/j.bmcl.2017.10.037

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