کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1356968 | 981184 | 2006 | 18 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
Tissue factor/factor VIIa complex (TF/FVIIa) inhibitors that contain a neutral P1 ligand were prepared and evaluated for inhibitory activity against TF/FVIIa in vitro.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 23, 1 December 2006, Pages 7688–7705
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 23, 1 December 2006, Pages 7688–7705
نویسندگان
Masanori Miura, 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,