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.

中文翻译：

---

发现含有十氢喹啉、十氢-1,6-萘啶或八氢-1H-吡咯并[3,2-c]吡啶支架的IDO1抑制剂

一系列含有十氢喹啉、十氢-1,6-萘啶或八氢-1H-吡咯并[3,2-c]吡啶支架的IDO1抑制剂被鉴定出对IDO1具有良好的细胞和人类全血活性。这些抑制剂包含多个手性中心，所有非对映异构体都被分离。未确定每种异构体的绝对立体化学。化合物15和27因其良好的细胞和人全血 IDO1 抑制活性、低未结合清除率和在大鼠盒 PK 研究中合理的平均停留时间而脱颖而出。