Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2017.10.037 | DOI Listing |
Publication Analysis
Top Keywords
pparδ modulator
8
novel highly
4
highly selective
4
selective peroxisome
4
peroxisome proliferator-activated
4
proliferator-activated receptor
4
receptor pparδ
4
pparδ modulators
4
modulators pharmacokinetic
4
pharmacokinetic properties
4
Similar Publications
Peroxisomal proliferator-activated receptor α-b deficiency induces the reprogramming of nutrient metabolism in zebrafish.
J Physiol
October 2020
LANEH, School of Life Sciences, East China Normal University, Shanghai, China.
Article Synopsis
- The pparab subtype in zebrafish is strongly expressed in high oxidative tissues and its deficiency reduces fatty acid β-oxidation in both liver and muscle, similar to the role of PPARα in mammals.
- Knockout of pparab leads to increased glucose utilization and inhibited amino acid breakdown, showcasing a metabolic shift in energy sources.
- This research offers new insights into PPARα's regulatory role in nutrient metabolism and establishes zebrafish as a valuable model for studying metabolic processes comparably to mammals.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!