Abstract
Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPARgamma ligand binding domain is described.
Copyright 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Angiotensin-Converting Enzyme Inhibitors / chemistry
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Angiotensin-Converting Enzyme Inhibitors / pharmacology
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Animals
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology
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Benzoates / chemistry
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Benzoates / pharmacology
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Crystallography, X-Ray
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Drug Design*
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Humans
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Structure
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PPAR gamma / drug effects*
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Rats
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Structure-Activity Relationship
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Telmisartan
Substances
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Angiotensin-Converting Enzyme Inhibitors
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Benzimidazoles
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Benzoates
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Indoles
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PPAR gamma
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Telmisartan