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Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.

作者信息

Phillips G B, Buckman B O, Davey D D, Eagen K A, Guilford W J, Hinchman J, Ho E, Koovakkat S, Liang A, Light D R, Mohan R, Ng H P, Post J M, Shaw K J, Smith D, Subramanyam B, Sullivan M E, Trinh L, Vergona R, Walters J, White K, Whitlow M, Wu S, Xu W, Morrissey M M

机构信息

Discovery Research, Berlex Biosciences, 15049 San Pablo Avenue, P.O. Box 4099, Richmond, California 94804-0099, USA.

出版信息

J Med Chem. 1998 Sep 10;41(19):3557-62. doi: 10.1021/jm980280h.

DOI:10.1021/jm980280h
PMID:9733480
Abstract
摘要

相似文献

1
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.N-[2-[5-[氨基（亚氨基）甲基]-2-羟基苯氧基]-3,5-二氟-6-[3-(4,5-二氢-1-甲基-1H-咪唑-2-基)苯氧基]吡啶-4-基]-N-甲基甘氨酸（ZK-807834）的发现：一种强效、选择性且口服活性的凝血酶因子Xa抑制剂。
J Med Chem. 1998 Sep 10;41(19):3557-62. doi: 10.1021/jm980280h.
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(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.
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Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.2,6 - 二苯氧基吡啶衍生的凝血因子Xa抑制剂的设计、合成及活性
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Discovery of the factor Xa inhibitor, ZK 807834 (CI-1031).凝血因子Xa抑制剂ZK 807834（CI-1031）的发现。
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Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.基于P1位2,5-噻吩脒的有效且口服生物可利用的凝血酶抑制剂：N-羧甲基-d-二苯基丙氨酰-l-脯氨酰[(5-脒基-2-噻吩基)甲基]酰胺的发现。
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Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.新型Xa因子抑制剂的合理设计、合成及构效关系：(2-取代-4-脒基苯基)丙酮酸和丙酸
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Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.凝血因子Xa强效和选择性抑制剂的设计及其构效关系
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Increased local expression of coagulation factor X contributes to the fibrotic response in human and murine lung injury.
凝血因子X在局部的表达增加会导致人和小鼠肺损伤中的纤维化反应。
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