Design, synthesis, and biological evaluation of 1,3-dioxoisoindoline-5-carboxamide derivatives as T-type calcium channel blockers

A small molecule library of 1,3-dioxoisoindoline-5-carboxamides 4 was designed based on the pharmacophore model, synthesized and biologically evaluated as potential T-type calcium channel blockers. The most active compounds 4d and 4n show T-type calcium channel blocking activity with IC50 values of 0.93 and 0.96 μM, respectively.

A small molecule library of 1,3-dioxoisoindoline-5-carboxamides 4 was designed, synthesized, and biologically evaluated as potential T-type calcium channel blockers. The most active compound shows blocking activity with IC50 value of 0.93 μM.Figure optionsDownload as PowerPoint slide