Issue 1, 2013

Optimization of triazole-based TGR5 agonists towards orally available agents

Abstract

Reported herein is a medicinal chemistry effort towards the identification of orally available TGR5 agonist 12, which served as a dog tool compound for studies to increase confidence in this mechanism. With the challenge of striking the balance of TGR5 potency and desired clearance profile, the screening strategy as well as medicinal chemistry strategy are discussed in this article.

Graphical abstract: Optimization of triazole -based TGR5 agonists towards orally available agents

Supplementary files

Article information

Article type
Concise Article
Submitted
30 Jun 2012
Accepted
31 Aug 2012
First published
26 Sep 2012

Med. Chem. Commun., 2013,4, 205-210

Optimization of triazole-based TGR5 agonists towards orally available agents

K. Futatsugi, K. B. Bahnck, M. B. Brenner, J. Buxton, J. E. Chin, S. B. Coffey, J. Dubins, D. Flynn, D. Gautreau, A. Guzman-Perez, J. R. Hadcock, D. Hepworth, M. Herr, T. Hinchey, A. M. Janssen, S. M. Jennings, W. Jiao, S. Y. Lavergne, B. Li, M. Li, M. J. Munchhof, S. T. M. Orr, D. W. Piotrowski, N. S. Roush, M. Sammons, B. D. Stevens, G. Storer, J. Wang, J. S. Warmus, L. Wei and A. C. Wolford, Med. Chem. Commun., 2013, 4, 205 DOI: 10.1039/C2MD20174G

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