Abstract
TGR5 agonists are potential therapeutics for a variety of conditions including type 2 diabetes, obesity, and inflammatory bowel disease. After screening a library of chenodeoxycholic acid (CDCA) derivatives, it was determined that a range of modifications could be made to the acid moiety of CDCA which significantly increased TGR5 agonist potency. Surprisingly, methylation of the 7-hydroxyl of CDCA led to a further dramatic increase in potency, allowing the identification of 5.6 nM TGR5 agonist 17.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 6824-6830 |
| Number of pages | 7 |
| Journal | Journal of medicinal chemistry |
| Volume | 62 |
| Issue number | 14 |
| DOIs | |
| State | Published - Jul 25 2019 |
Bibliographical note
Publisher Copyright:© 2019 American Chemical Society.
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