GlaxoSmithKline, 5 Moore Drive, P.O. Box 13398, Research Triangle Park, NC 27709, United States.
GlaxoSmithKline, 5 Moore Drive, P.O. Box 13398, Research Triangle Park, NC 27709, United States.
Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13.
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imidazopyridine inhibitor of H-PGDS, 20b. Herein, describes the identification of 2 classes of inhibitors, their syntheses, and their challenges.
通过葛兰素史克公司内部的虚拟屏幕，发现了一类独特的 2-苯基咪唑并[1,2-a]吡啶-6-甲酰胺 H-PGDS 抑制剂。对晶体结构和 SAR 的仔细评估导致了一种新型的、有效的、具有口服活性的 H-PGDS 咪唑并吡啶抑制剂 20b。本文描述了两类抑制剂的鉴定、它们的合成以及它们所面临的挑战。
