取代的哌啶作为 HDM2 抑制剂。
Substituted piperidines as HDM2 inhibitors.
机构信息
Discovery and Preclinical Sciences, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, United States.
Discovery and Preclinical Sciences, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, United States.
出版信息
Bioorg Med Chem Lett. 2014 Feb 15;24(4):1026-30. doi: 10.1016/j.bmcl.2014.01.026. Epub 2014 Jan 17.
Novel small molecule HDM2 inhibitor, substituted piperidine, was identified. Initial SAR study indicated potential for several position optimizations. Additional potency enhancement was achieved by introducing a sidechain off the aromatic ring. DMPK study of one of the active compounds has shown a moderate oral PK and reasonable bioavailability.
新型小分子 HDM2 抑制剂，取代哌啶，被鉴定出来。初步 SAR 研究表明有几个位置具有优化潜力。通过在芳环上引入侧链，进一步提高了化合物的活性。其中一个活性化合物的 DMPK 研究表明其具有中等的口服 PK 和合理的生物利用度。
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