144060-69-5Relevant academic research and scientific papers
Synthesis and evaluation of sulfonylnitrophenylthiazoles (SNPTs) as thyroid hormone receptor-coactivator interaction inhibitors
Hwang, Jong Yeon,Attia, Ramy R.,Zhu, Fangyi,Yang, Lei,Lemoff, Andrew,Jeffries, Cynthia,Connelly, Michele C.,Guy, R. Kiplin
, p. 2301 - 2310 (2012/05/21)
We previously identified a series of methylsulfonylnitrobenzoates (MSNBs) that block the interaction of the thyroid hormone receptor with its coactivators. MSNBs inhibit coactivator binding through irreversible modification of cysteine 298 of the thyroid hormone receptor (TR). Although MSNBs have better pharmacological features than our first generation inhibitors (β-aminoketones), they contain a potentially unstable ester linkage. Here we report the bioisosteric replacement of the ester linkage with a thiazole moiety, yielding sulfonylnitrophenylthiazoles (SNPTs). An array of SNPTs representing optimal side chains from the MSNB series was constructed using parallel chemistry and evaluated to test their antagonism of the TR-coactivator interaction. Selected active compounds were evaluated in secondary confirmatory assays including regulation of thyroid response element driven transcription in reporter constructs and native genes. In addition the selected SNPTs were shown to be selective for TR relative to other nuclear hormone receptors (NRs).
2-arylthiazole derivatives and pharmaceutical composition thereof
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, (2008/06/13)
Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): STR1 wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group; X is a hydrogen atom, alkyl group or carboxyl group which may be protected, and Y is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected. Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.
