59893-99-1Relevant articles and documents
Addressing hERG activity while maintaining favorable potency, selectivity and pharmacokinetic properties of PPARδ modulators
Lagu, Bharat,Senaiar, Ramesh S.,Kluge, Arthur F.,Mallesh,Ramakrishna,Bhat, Raveendra,Patane, Michael A.
, (2020)
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.
PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Page/Page column 44-45, (2017/11/10)
Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Magnetic CuFe2O4 nanoparticles: A retrievable catalyst for oxidative amidation of aldehydes with amine hydrochloride salts
Suresh Kumar,Thulasiram,Bala Laxmi,Rawat, Vikas S.,Sreedhar
supporting information, p. 6059 - 6067 (2015/03/30)
The application of magnetic CuFe2O4 nanoparticles for the oxidative amidation of aldehydes with amine hydrochloride salts is described. A wide range of amides have been synthesized in good to excellent yields under mild conditions. Chiral amide also synthesized from its corresponding chiral amine salt with retention of the stereochemistry. In particular, the performance of the magnetic separation of the catalyst was very efficient and an alternative to time, solvent and energy-consuming separation procedures. The catalytic activity of the catalyst remains unaltered after five consecutive cycles, making it environmentally benign and widely applicable due to its efficiency, ease of handling and cost effectiveness.