Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors

Glunz Peter W.; Cheng Xuhong; Cheney Daniel L.Weigelt Carolyn A.Wei AnzhiLuettgen Joseph M.Wong Pancras C.Wexler Ruth R.Priestley E. Scott

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Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors

机译：基于苯基咪唑的强效选择性苯基咪唑FVIIa抑制剂的设计和合成

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Heterocyclic amide isosteres were incorporated into a phenylglycine-based tissue factor/factor VIIa (TF-FVIIa) inhibitor chemotype, providing potent inhibitors. An X-ray co-crystal structure of phenylimidazole 19 suggested that an imidazole nitrogen atom effectively mimics an amide carbonyl, while the phenyl ring forms key hydrophobic interactions with the S-1' pocket. Exploration of phenylimidazole substitution led to the discovery of potent, selective and efficacious inhibitors of TF-FVIIa. (C) 2015 Elsevier Ltd. All rights reserved.

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2015年第10期|2169-2173|共5页
作者
Glunz Peter W.; Cheng Xuhong; Cheney Daniel L.Weigelt Carolyn A.Wei AnzhiLuettgen Joseph M.Wong Pancras C.Wexler Ruth R.Priestley E. Scott;
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作者单位

Bristol Myers Squibb R&D, Pennington, NJ 08534 USA;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Factor VIIa; Tissue factor; TF-FVIIa inhibitor; Serine protease inhibitors; Amide isosteres;

机译：因子 VIIa;组织因子;TF-FVIIa 抑制剂;丝氨酸蛋白酶抑制剂;酰胺等固醇;

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Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors

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