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Title: Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors

Abstract

Using structure based drug design, novel aminobenzisoxazoles as coagulation factor IXa inhibitors were designed and synthesized. Highly selective inhibition of FIXa over FXa was demonstrated. Anticoagulation profile of selected compounds was evaluated by aPTT and PT tests. In vitro ADMET and pharmacokinetic (PK) profiles were also evaluated.

Authors:
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Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
USDOE
OSTI Identifier:
1404976
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorganic and Medicinal Chemistry Letters; Journal Volume: 27; Journal Issue: 11
Country of Publication:
United States
Language:
ENGLISH
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY; 60 APPLIED LIFE SCIENCES

Citation Formats

Sakurada, Isao, Endo, Toshiya, Hikita, Katsuyoshi, Hirabayashi, Tomokazu, Hosaka, Yoshitaka, Kato, Yutaka, Maeda, Yoshitaka, Matsumoto, Shigeki, Mizuno, Takashi, Nagasue, Hiroshi, Nishimura, Teruyuki, Shimada, Shunsuke, Shinozaki, Mikihiko, Taguchi, Keiko, Takeuchi, Katsutoshi, Yokoyama, Tooru, Hruza, Alan, Reichert, Paul, Zhang, Ting, Wood, Harold B., Nakao, Kazunari, and Furusako, Shoji. Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors. United States: N. p., 2017. Web. doi:10.1016/j.bmcl.2017.03.002.
Sakurada, Isao, Endo, Toshiya, Hikita, Katsuyoshi, Hirabayashi, Tomokazu, Hosaka, Yoshitaka, Kato, Yutaka, Maeda, Yoshitaka, Matsumoto, Shigeki, Mizuno, Takashi, Nagasue, Hiroshi, Nishimura, Teruyuki, Shimada, Shunsuke, Shinozaki, Mikihiko, Taguchi, Keiko, Takeuchi, Katsutoshi, Yokoyama, Tooru, Hruza, Alan, Reichert, Paul, Zhang, Ting, Wood, Harold B., Nakao, Kazunari, & Furusako, Shoji. Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors. United States. doi:10.1016/j.bmcl.2017.03.002.
Sakurada, Isao, Endo, Toshiya, Hikita, Katsuyoshi, Hirabayashi, Tomokazu, Hosaka, Yoshitaka, Kato, Yutaka, Maeda, Yoshitaka, Matsumoto, Shigeki, Mizuno, Takashi, Nagasue, Hiroshi, Nishimura, Teruyuki, Shimada, Shunsuke, Shinozaki, Mikihiko, Taguchi, Keiko, Takeuchi, Katsutoshi, Yokoyama, Tooru, Hruza, Alan, Reichert, Paul, Zhang, Ting, Wood, Harold B., Nakao, Kazunari, and Furusako, Shoji. Thu . "Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors". United States. doi:10.1016/j.bmcl.2017.03.002.
@article{osti_1404976,
title = {Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors},
author = {Sakurada, Isao and Endo, Toshiya and Hikita, Katsuyoshi and Hirabayashi, Tomokazu and Hosaka, Yoshitaka and Kato, Yutaka and Maeda, Yoshitaka and Matsumoto, Shigeki and Mizuno, Takashi and Nagasue, Hiroshi and Nishimura, Teruyuki and Shimada, Shunsuke and Shinozaki, Mikihiko and Taguchi, Keiko and Takeuchi, Katsutoshi and Yokoyama, Tooru and Hruza, Alan and Reichert, Paul and Zhang, Ting and Wood, Harold B. and Nakao, Kazunari and Furusako, Shoji},
abstractNote = {Using structure based drug design, novel aminobenzisoxazoles as coagulation factor IXa inhibitors were designed and synthesized. Highly selective inhibition of FIXa over FXa was demonstrated. Anticoagulation profile of selected compounds was evaluated by aPTT and PT tests. In vitro ADMET and pharmacokinetic (PK) profiles were also evaluated.},
doi = {10.1016/j.bmcl.2017.03.002},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 11,
volume = 27,
place = {United States},
year = {Thu Jun 01 00:00:00 EDT 2017},
month = {Thu Jun 01 00:00:00 EDT 2017}
}