1. Aza-Retinoids as Novel Retinoid X Receptor-Specific Agonists
- Author
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Chan Hwang, Youssef L. Bennani, Kristen S. Marron, Luc J. Farmer, Stacie S. Canan Koch, Alex M. Nadzan, E. Adam Kallel, Dave W. Robertson, and Zhi Lin
- Subjects
Agonist ,Tertiary amine ,medicine.drug_class ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Retinoid X receptor ,Biochemistry ,Chemical synthesis ,Retinoids ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Structure–activity relationship ,Retinoid ,RXR activity ,Molecular Biology ,Aza Compounds ,Molecular Structure ,Chemistry ,Organic Chemistry ,Stereoisomerism ,General Medicine ,In vitro ,body regions ,Chain length ,Retinoid X Receptors ,Molecular Medicine ,lipids (amino acids, peptides, and proteins) - Abstract
A new structurally simple series of potent lipophilic aza-retinoids RXR agonists has been developed. SAR studies for the N-alkyl-azadienoic acids described here demonstrate that the RXR activity profile is sensitive to the N-alkyl chain length. Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series.
- Published
- 2006