Parallel Synthesis of a Biased Library of Thiazolidinones as Novel Sodium Channel Antagonists

Title: Parallel Synthesis of a Biased Library of Thiazolidinones as Novel Sodium Channel Antagonists

Volume: 6 Issue: 5

Author(s): Qun Sun, Laykea Tafesse, James T. Limberis, Khondekar Islam and Donald J. Kyle

Affiliation:

Keywords: parallel synthesis, biased library of thiazolidinones, novel sodium channel antagonists, anticonvulsant agent, sodium channel antagonism

Abstract: A biased chemical library containing 91 differentially substituted thiazolidinones was prepared in an effort to improve the pharmacology of a known anticonvulsant agent V102862. The collection was prepared in a single step multi-component condensation reaction that produced good yields and very high crude purity (75%-85%). Seven compounds, identified within the library were shown to be more potent than V102862, our parent reference compound, in an electrophysiological assay measuring sodium channel antagonism. The most potent compound, 3-(2-piperidinylethyl)-2-(3-(3-trifluoromethylphenoxy)phenyl)thiazolidinone, has a Ki of 90 nM.

Cite this article as:

Sun Qun, Tafesse Laykea, Limberis T. James, Islam Khondekar and Kyle J. Donald, Parallel Synthesis of a Biased Library of Thiazolidinones as Novel Sodium Channel Antagonists, Combinatorial Chemistry & High Throughput Screening 2003; 6 (5) . https://dx.doi.org/10.2174/138620703106298653