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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amides / chemistry*
-
Amides / pharmacology*
-
Calcium Channel Blockers / chemical synthesis*
-
Calcium Channel Blockers / pharmacology*
-
Calcium Channels, T-Type / drug effects*
-
Cell Line
-
Crystallography, X-Ray
-
Dose-Response Relationship, Drug
-
Drug Design
-
Humans
-
Indicators and Reagents
-
Indoles / chemistry*
-
Indoles / pharmacology*
-
Membrane Potentials / drug effects
-
Mibefradil / pharmacology
-
Models, Molecular
-
Patch-Clamp Techniques
Substances
-
1,3-dioxoisoindoline-5-carboxamide
-
Amides
-
Calcium Channel Blockers
-
Calcium Channels, T-Type
-
Indicators and Reagents
-
Indoles
-
Mibefradil