Preparation and Pharmacological Evaluation of Novel Glycoprotein (Gp) IIb/IIIa Antagonists. 1. The Selection of Naphthalene Derivatives

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概要

• 論文の詳細を見る

• The synthesis and design using molecular modeling techniques for non-peptide, low molecular weight novel fibrinogen receptor (glycoprotein IIb/IIIa : Gp IIb/IIIa) antagonists, is reported. We used a highly potent serine protease inhibitor, Nafamostat, having an amidinonaphthyl unit as the starting compound. The compounds 4-(6-amidino-2-naphthylaminocarbonyl)phenoxyacetic acid (5a) and 4-(6-amidino-2-naphthalenecarboxamido)phenoxyacetic acid (5b) inhibited adenosin-5'-diphospate (ADP)-induced aggregation of human platelet-rich plasma (PRP) with IC_<50> values of 0.05 and 0.07 μM, respectively, and had lost their ability to inhibit a variety of serine proteases, including thrombin, factor Xa, plasmin and trypsin.

• 公益社団法人日本薬学会の論文
• 1999-12-15

著者

• Isobe Y

  Research Division Discovery Research Laboratories Ii Sumitomo Pharmaceuticals Co. Ltd.

• Fukaya C

  Yoshitomi Pharmaceutical Ind. Ltd. Osaka Jpn

• Fukaya Chikara

  Quality Control Production Division Yoshitomi Pharmaceutical Industries Ltd.

• Yoshida Tomohiro

  Exploratory Research Ii Drug Discovery Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• Nakamura Norifumi

  President's Office Yoshitomi Pharmaceutical Industries Ltd.

• Nakamura Norihiro

  Department Of Biological Sciences Graduate School Of Science Osaka University

• 五十部 穣

  Research Center Sumitomo Pharmaceuticals Co. Ltd.

• Inoue Y

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• KOSAKA Keigo

  Enabling Technologies, Drug Discovery Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• INOUE Yoshihisa

  Enabling Technologies, Drug Discovery Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• IMADA Teruaki

  Exploratory Research II Drug Discovery Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• ASHIMORI Atsuyuki

  Exploratory Research II Drug Discovery Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.,

• Kosaka K

  Beauty Care Products Division Health Care Business Group Nagase & Co. Ltd.

• Imada T

  Mitsubishi Pharma Corp. Yokohama Jpn

• Inoue Y

  Osaka Univ. Osaka Jpn

• Yoshida T

  Hakodate Institute Of National College Of Technology

• Ashimori A

  Exploratory Research Ii Drug Discovery Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• Ono Shin'ichiro

  Exploratory Research Ii Drug Discovery Laboratories Yoshitomi Pharmaceutical Industries Ltd.

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