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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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

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

Volume 6, Issue 5, 2003

Page: [481 - 488] Pages: 8

DOI: 10.2174/138620703106298653

Price: $65


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.

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

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