Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
3 years ago

Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold

Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-<em>c</em>]pyridine scaffold
Wensheng Yu, Yongqi Deng, David Sloman, Derun Li, Kun Liu, Xavier Fradera, Charles A. Lesburg, Theo Martinot, Amy Doty, Heidi Ferguson, J. Richard Miller, Ian Knemeyer, Karin Otte, Stella Vincent, Nunzio Sciammetta, David Jonathan Bennett, Yongxin Han

A series of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold were identified with good cellular and human whole blood activity against IDO1. These inhibitors contain multiple chiral centers and all diastereomers were separated. The absolute stereochemistry of each isomers were not determined. Compounds 15 and 27 stood out as leads due to their good cellular as well as human whole blood IDO1 inhibition activity, low unbound clearance, and reasonable mean residence time in rat cassette PK studies.

Publisher URL: https://www.sciencedirect.com/science/article/pii/S0960894X21005412

DOI: 10.1016/j.bmcl.2021.128314

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