4-氨基嘧啶四氢萘酚：一系列具有改善溶解性的新型香草酸受体-1拮抗剂。
4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.
作者信息
Doherty Elizabeth M, Retz Daniel, Gavva Narender R, Tamir Rami, Treanor James J S, Norman Mark H
机构信息
Department of Chemistry Research and Discovery, One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1830-4. doi: 10.1016/j.bmcl.2008.02.022. Epub 2008 Feb 13.
8-(6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol (4) and analogs (5-10) were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility over our previous series. Synthesis, SAR, and improvements in metabolic stability and absorption of these compounds are described herein.
8 -（6 -（4 -（三氟甲基）苯基）嘧啶 - 4 - 基氨基）- 1,2,3,4 - 四氢萘 - 2 - 醇（4）及其类似物（5 - 10）在体外被证明是人和大鼠TRPV1的有效抑制剂，且与我们之前的系列相比溶解度有所提高。本文描述了这些化合物的合成、构效关系以及代谢稳定性和吸收方面的改进。
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