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PDBsum entry 6izn
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Transcription
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PDB id
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6izn
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References listed in PDB file
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Key reference
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Title
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Structure-Activity relationship studies of 3- Or 4-Pyridine derivatives of ds-6930.
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Authors
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T.Shinozuka,
T.Tsukada,
K.Fujii,
E.Tokumaru,
Y.Matsui,
S.Wakimoto,
T.Ogata,
K.Araki,
R.Sawamura,
N.Watanabe,
M.Mori,
J.Tanaka.
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Ref.
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ACS Med Chem Lett, 2019,
10,
358-362.
[DOI no: ]
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PubMed id
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Abstract
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Derivatization efforts were continued to discover backups for a potent selective
PPARĪ³ modulator, DS-6930. In this Letter, the replacement of 2-pyridine ring in
DS-6930 with 3- or 4-pyridyl group is reported. As the introduction of
substituents on the pyridine ring did not provide potent partial agonists,
modifications of benzimidazole ring were explored to discover potent
intermediate agonists. 4'-Alkoxy substituted benzimidazoles failed to show
potent efficacy in vivo, whereas 7'-fluoro benzimidazole 3g (DS19161384)
was found to result in robust plasma glucose reductions with excellent DMPK
profiles.
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