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2020 - Addressing hERG activity while maintaining favorable potency, selectivity and pharmacokinetic properties of PPARδ modulators

icon pap   Port-a Patch Publication in Bioorganic & Medicinal Chemistry Letters (2020)

Authors:
Lagu B., Senaiar R.S., Kluge A.F., Mallesh B., Ramakrishna M., Bhat R., Patane M.A.

Journal:
Bioorganic & Medicinal Chemistry Letters (2020) 30(4): Article 126928


Abstract:

One of the most commonly used strategies to reduce hERG (human ether-a-go-go) activity in the drug candidates is introduction of a carboxylic acid group. During the optimization of PPARδ modulators, some of the compounds containing a carboxylic acid were found to inhibit the hERG channel in a patch clamp assay. By modifying the basicity of the imidazole core, potent and selective PPARδ modulators that do not inhibit hERG channel were identified. Some of the modulators have excellent pharmacokinetic profiles in mice.


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