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  • Title: Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase.
    Author: Eldrup AB, Soleymanzadeh F, Farrow NA, Kukulka A, De Lombaert S.
    Journal: Bioorg Med Chem Lett; 2010 Jan 15; 20(2):571-5. PubMed ID: 19969453.
    Abstract:
    Inhibition of sEH is hypothesized to lead to an increase in epoxyeicosatrienoic acids resulting in the potentiation of their anti-inflammatory and vasodilatory effects. In an effort to explore sEH inhibition as an avenue for the development of vasodilatory and cardio- or renal-protective agents, a lead identified through high-throughput screening was optimized, guided by the determination of a solid state co-structure with sEH. Replacement of potential toxicophores was followed by optimization of cell-based potency and ADME properties to provide a new class of functionally potent sEH inhibitors with attractive in vitro metabolic profiles and high and sustained plasma exposures after oral administration in the rat.
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