期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 24, 页码 7958-7961出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm901390p
关键词
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资金
- Intercept Pharmaceuticals (New York, NY)
- ANR PHYSIO (BASE)
- EU (Eugene2)
- EFPL
- SNF
In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C-23(S)methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords selectivity for TGR5. Herein we report further lead optimization efforts that have led to the discovery of 6 alpha-ethyl-23(S)-methylcholic acid (S-EMCA. INT-777)as a novel Potent and selective TGR5 agonist with remarkable in vivo activity.
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