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

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Kim HS, Kim Y, Doddareddy MR, Seo SH, Rhim H, Tae J, Pae AN, Choo H, Cho YS

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

Bioorg Med Chem Lett. 2007 Jan 15;17(2):476-81. Epub 2006 Oct 21.

PubMed ID

17092715 [ View in PubMed

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Abstract

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 microM, respectively.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mibefradil	Voltage-dependent T-type calcium channel subunit alpha-1G	IC 50 (nM)	1340	N/A	N/A	Details