Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands

PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate (AMC) template. PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate template. Several compounds in this series have demonstrat...

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Published inBioorganic & medicinal chemistry letters Vol. 16; no. 24; pp. 6328 - 6333
Main Authors Warshawsky, Alan M., Alt, Charles A., Brozinick, Joseph T., Harkness, Allen R., Hawkins, Eric D., Henry, James R., Matthews, Donald P., Miller, Anne R., Misener, Elizabeth A., Montrose-Rafizadeh, Chahrzad, Rhodes, Gary A., Shen, Quanrong, Vance, Jennifer A., Udodong, Uko E., Wang, Minmin, Zhang, Tony Y., Zink, Richard W.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 15.12.2006
Elsevier
Subjects
Biological and medical sciences
Cinnamates - chemical synthesis
Cinnamates - pharmacokinetics
General and cellular metabolism. Vitamins
Humans
Hypoglycemic Agents - therapeutic use
Ligands
Medical sciences
Peroxisome Proliferator-Activated Receptors - physiology
Pharmacology. Drug treatments
PPAR
PPAR alpha - physiology
PPAR gamma - physiology
Structure-Activity Relationship
Thiazolidinediones - chemical synthesis
Thiazolidinediones - therapeutic use
PPAR
Endocrinopathy
Type 2 diabetes
Nuclear receptor
Rat
Ligand
Thiazole derivatives
Selectivity
Hypoglycemic agent
Structure activity relation
Carboxylic acid
Arylpropionic acid derivatives
Chemical synthesis
Oxazole derivatives
Peroxisome proliferator activated receptor
Rodentia
Benzene derivatives
Oral administration
Metabolic diseases
Triglyceride
In vitro
In vivo
Vertebrata
Chemotherapy
Biological fixation
Experimental disease
Mammalia
Treatment
Mouse
Animal
Affinity
Antilipemic agent
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Summary:PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate (AMC) template. PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate template. Several compounds in this series have demonstrated potent plasma glucose and triglyceride lowering capability in rodent models of type 2 diabetes.
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ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.09.011