Literature DB >> 16942884

Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand.

Masanori Miura1, Norio Seki, Takanori Koike, Tsukasa Ishihara, Tatsuya Niimi, Fukushi Hirayama, Takeshi Shigenaga, Yumiko Sakai-Moritani, Tomihisa Kawasaki, Shuichi Sakamoto, Minoru Okada, Mitsuaki Ohta, Shin-ichi Tsukamoto.   

Abstract

Inhibition of tissue factor/factor VIIa complex (TF/FVIIa) is an attractive strategy for antithrombotic therapies. We began with an investigation of a non-amidine TF/FVIIa inhibitor based on a modification of amidine compound 1. Optimization of the substituents on the P1 phenyl portion of the compound 1 led to a neutral or less basic alternative for the 4-amidinophenyl moiety. By further optimization of the substituents on the central phenyl ring, a highly potent and selective TF/FVIIa inhibitor 17d was discovered.

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Year:  2006        PMID: 16942884     DOI: 10.1016/j.bmc.2006.08.010

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

1.  Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.

Authors:  Nicholas R Wurtz; Brandon L Parkhurst; Wen Jiang; Indawati DeLucca; Xiaojun Zhang; Vladimir Ladziata; Daniel L Cheney; Jeffrey R Bozarth; Alan R Rendina; Anzhi Wei; Joseph M Luettgen; Yiming Wu; Pancras C Wong; Dietmar A Seiffert; Ruth R Wexler; E Scott Priestley
Journal:  ACS Med Chem Lett       Date:  2016-09-17       Impact factor: 4.345

  1 in total

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