Successful reduction of off-target hERG toxicity by structural modification of a T-type calcium channel blocker was written by Choi, Yeon Jae;Seo, Jae Hong;Shin, Kye Jung. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Application of 1061284-70-5 The following contents are mentioned in the article:
To obtain an optimized T-type calcium channel blocker with reduced off-target hERG toxicity, we modified the structure of the original compound by introducing a zwitterion and reducing the basicity of the nitrogen. Among the structurally modified compounds we designed, compounds 5 and 6, which incorporate amides in place of the original compound’s amines, most appreciably alleviated hERG toxicity while maintaining T-type calcium channel blocking activity. Notably, the benzimidazole amide 5 selectively blocked T-type calcium channels without inhibiting hERG (hERG/T-type â?220) and L-type channels (L-type/T-type = 96), and exhibited an excellent pharmacokinetic profile in rats. This study involved multiple reactions and reactants, such as Methyl 2-(4-bromophenyl)-3-methylbutanoate (cas: 1061284-70-5Application of 1061284-70-5).
Methyl 2-(4-bromophenyl)-3-methylbutanoate (cas: 1061284-70-5) belongs to esters. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.Application of 1061284-70-5
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics