具有苯并噻吩药效团的强效和选择性 5-LO 抑制剂：MK-5286 的发现。
Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286.
机构信息
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada.
出版信息
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7440-3. doi: 10.1016/j.bmcl.2010.10.024. Epub 2010 Oct 15.
PMID:21044840
Abstract
The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1H-1,2,3-triazol-1-yl}methyl)-1-benzothiophene-2-carboxamide ((S)-2l or MK-5286) were described.
摘要
本文描述了一种新型强效、可口服的 5-脂氧合酶（5-LO）抑制剂 3-（4-氟苯基）-6-({4-[(1S)-1-羟基-1-（三氟甲基）丙基]-1H-1,2,3-三唑-1-基}甲基）-1-苯并噻吩-2-甲酰胺（（S）-2l 或 MK-5286）的发现策略和 SAR 研究。
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