GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
J Med Chem. 2022 Feb 10;65(3):1767-1769. doi: 10.1021/acs.jmedchem.1c02108. Epub 2021 Dec 28.
Over the past two decades, Factor XIa inhibitors have emerged as an exciting new class of antithrombic agents. Identification of orally bioavailable small molecule inhibitors has presented a formidable challenge for medicinal chemists. Herein, those challenges and the problem-solving that resulted in the discovery of milvexian will be presented.
在过去的二十年中,因子 XIa 抑制剂已成为一类令人兴奋的新型抗血栓形成药物。鉴定口服生物利用的小分子抑制剂对药物化学家来说是一个巨大的挑战。本文将介绍这些挑战以及在发现米伏先的过程中解决这些挑战的方法。